Giuseppe Campiani

Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation.

ACS Med Chem Lett 2020 Nov 29;11(11):2268-2276. Epub 2020 Sep 29.

Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, I-53100 Siena, Italy.

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November 2020

Novel quinolone-based potent and selective HDAC6 inhibitors: Synthesis, molecular modeling studies and biological investigation.

Authors:

Nicola Relitti A Prasanth Saraswati Giulia Chemi Margherita Brindisi Simone Brogi Daniel Herp Karin Schmidtkunz Fulvio Saccoccia Giovina Ruberti Cristina Ulivieri Francesca Vanni Federica Sarno Lucia Altucci Stefania Lamponi Manfred Jung Sandra Gemma Stefania Butini Giuseppe Campiani

Eur J Med Chem 2020 Nov 7:112998. Epub 2020 Nov 7.

Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy. Electronic address:

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November 2020

Cinnamides Target Arginase Selectively.

Authors:

Edson Roberto da Silva Júlio Abel Alfredo Dos Santos Simone Come Simone Brogi Vincenzo Calderone Giulia Chemi Giuseppe Campiani Trícia Maria Ferrreira de Sousa Oliveira Thanh-Nhat Pham Marc Pudlo Corine Girard Claudia do Carmo Maquiaveli

Molecules 2020 Nov 12;25(22). Epub 2020 Nov 12.

Laboratório de Farmacologia e Bioquímica (LFBq), Departamento de Medicina Veterinária, Universidade de São Paulo Faculdade de Zootecnia e Engenharia de Alimentos, Pirassununga, SP 13635-900, Brazil.

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November 2020

Selective Histone Deacetylase 6 Inhibitors Restore Cone Photoreceptor Vision or Outer Segment Morphology in Zebrafish and Mouse Models of Retinal Blindness.

Authors:

Husvinee Sundaramurthi Sarah L Roche Guinevere L Grice Ailis Moran Eugene T Dillion Giuseppe Campiani James A Nathan Breandán N Kennedy

Front Cell Dev Biol 2020 26;8:689. Epub 2020 Aug 26.

UCD Conway Institute, University College Dublin, Dublin, Ireland.

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August 2020

Modulation of the Innate Immune Response by Targeting Toll-like Receptors: A Perspective on Their Agonists and Antagonists.

Authors:

Stefano Federico Luca Pozzetti Alessandro Papa Gabriele Carullo Sandra Gemma Stefania Butini Giuseppe Campiani Nicola Relitti

J Med Chem 2020 11 15;63(22):13466-13513. Epub 2020 Sep 15.

Department of Biotechnology, Chemistry and Pharmacy, Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100, Siena, Italy.

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November 2020

(+)-(R)- and (-)-(S)-Perhexiline maleate: Enantioselective synthesis and functional studies on Schistosoma mansoni larval and adult stages.

Authors:

Alessandra Guidi A Prasanth Saraswati Nicola Relitti Roberto Gimmelli Fulvio Saccoccia Carmina Sirignano Orazio Taglialatela-Scafati Giuseppe Campiani Giovina Ruberti Sandra Gemma

Bioorg Chem 2020 09 30;102:104067. Epub 2020 Jun 30.

Department of Biotechnology, Chemistry and Pharmacy, University of Siena, via Aldo Moro 2, 53100 Siena, Italy. Electronic address:

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September 2020

Retinitis Pigmentosa and Retinal Degenerations: Deciphering Pathways and Targets for Drug Discovery and Development.

Authors:

Gabriele Carullo Stefano Federico Nicola Relitti Sandra Gemma Stefania Butini Giuseppe Campiani

ACS Chem Neurosci 2020 08 9;11(15):2173-2191. Epub 2020 Jul 9.

Department of Biotechnology, Chemistry and Pharmacy, Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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August 2020

Ionotropic Glutamate Receptor GluA2 in Complex with Bicyclic Pyrimidinedione-Based Compounds: When Small Compound Modifications Have Distinct Effects on Binding Interactions.

Authors:

Karla Frydenvang Darryl S Pickering Giridhar U Kshirsagar Giulia Chemi Sandra Gemma Desiree Sprogøe Anne Mette Kærn Simone Brogi Giuseppe Campiani Stefania Butini Jette Sandholm Kastrup

ACS Chem Neurosci 2020 06 5;11(12):1791-1800. Epub 2020 Jun 5.

Department of Drug Design and Pharmacology, University of Copenhagen, Jagtvej 162, DK-2100 Copenhagen, Denmark.

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June 2020

Computer-Driven Development of an in Silico Tool for Finding Selective Histone Deacetylase 1 Inhibitors.

Authors:

Hajar Sirous Giuseppe Campiani Simone Brogi Vincenzo Calderone Giulia Chemi

Molecules 2020 Apr 22;25(8). Epub 2020 Apr 22.

Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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April 2020

Telomerase-based Cancer Therapeutics: A Review on their Clinical Trials.

Authors:

Nicola Relitti Akella P Saraswati Stefano Federico Tuhina Khan Margherita Brindisi Daniela Zisterer Simone Brogi Sandra Gemma Stefania Butini Giuseppe Campiani

Curr Top Med Chem 2020 ;20(6):433-457

Department of Biotechnology, Chemistry and Pharmacy, Department of Excellence 2018-2022, via Aldo Moro 2, I- 53100 Siena, University of Siena, Siena, Italy.

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December 2020

A Repurposing Approach for Uncovering the Anti-Tubercular Activity of FDA-Approved Drugs with Potential Multi-Targeting Profiles.

Authors:

Basem Battah Giulia Chemi Stefania Butini Giuseppe Campiani Simone Brogi Giovanni Delogu Sandra Gemma

Molecules 2019 Nov 29;24(23). Epub 2019 Nov 29.

Department of Biotechnology (DoE 2018-2022), Chemistry and Pharmacy (DoE 2018-2022), University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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November 2019

Autophagy modulators for the treatment of oral and esophageal squamous cell carcinomas.

Authors:

Tuhina Khan Nicola Relitti Margherita Brindisi Stefania Magnano Daniela Zisterer Sandra Gemma Stefania Butini Giuseppe Campiani

Med Res Rev 2020 05 19;40(3):1002-1060. Epub 2019 Nov 19.

Department of Biotechnology, Chemistry, and Pharmacy, Department of Excellence 2018-2022, University of Siena, Siena, Italy.

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May 2020

Screening and Phenotypical Characterization of Histone Deacetylase 8 (HDAC8) Inhibitors as Multistage Antischistosomal Agents.

Authors:

Fulvio Saccoccia Margherita Brindisi Roberto Gimmelli Nicola Relitti Alessandra Guidi A Prasanth Saraswati Caterina Cavella Simone Brogi Giulia Chemi Stefania Butini Giuliana Papoff Johanna Senger Daniel Herp Manfred Jung Giuseppe Campiani Sandra Gemma Giovina Ruberti

ACS Infect Dis 2020 01 12;6(1):100-113. Epub 2019 Nov 12.

Institute of Biochemistry and Cell Biology (IBBC) , National Research Council (CNR) , Campus A. Buzzati-Traverso, via E. Ramarini 32 , 00015 Monterotondo ( Rome ), Italy.

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January 2020

Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems.

Eur J Med Chem 2019 Dec 4;183:111674. Epub 2019 Sep 4.

Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100, Siena, Italy.

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December 2019

An integrated in silico screening strategy for identifying promising disruptors of p53-MDM2 interaction.

Authors:

Hajar Sirous Giulia Chemi Giuseppe Campiani Simone Brogi

Comput Biol Chem 2019 Dec 16;83:107105. Epub 2019 Aug 16.

Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126, Pisa, Italy.

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December 2019

Identification of Novel 3-Hydroxy-pyran-4-One Derivatives as Potent HIV-1 Integrase Inhibitors Using Structure-Based Combinatorial Library Design Approach.

Authors:

Hajar Sirous Giulia Chemi Sandra Gemma Stefania Butini Zeger Debyser Frauke Christ Lotfollah Saghaie Simone Brogi Afshin Fassihi Giuseppe Campiani Margherita Brindisi

Front Chem 2019 13;7:574. Epub 2019 Aug 13.

Department of Pharmacy, Department of Excellence 2018-2022, University of Naples Federico II, Naples, Italy.

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August 2019

Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.

Authors:

Margherita Brindisi A Prasanth Saraswati Simone Brogi Sandra Gemma Stefania Butini Giuseppe Campiani

J Med Chem 2020 01 27;63(1):23-39. Epub 2019 Aug 27.

Department of Biotechnology, Chemistry and Pharmacy, Department of Excellence 2018-2022 , University of Siena , via Aldo Moro 2 , 53100 , Siena , Italy.

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January 2020

Bridged bicyclic 2,3-dioxabicyclo[3.3.1]nonanes as antiplasmodial agents: Synthesis, structure-activity relationships and studies on their biomimetic reaction with Fe(II).

Authors:

Sarah D'Alessandro Gloria Alfano Luisa Di Cerbo Simone Brogi Giulia Chemi Nicola Relitti Margherita Brindisi Stefania Lamponi Ettore Novellino Giuseppe Campiani Sandra Gemma Nicoletta Basilico Donatella Taramelli Maria Camilla Baratto Rebecca Pogni Stefania Butini

Bioorg Chem 2019 08 31;89:103020. Epub 2019 May 31.

Department of Biotechnology, Chemistry and Pharmacy (DoE 2018-2022), University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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August 2019

Raising the bar in anticancer therapy: recent advances in, and perspectives on, telomerase inhibitors.

Authors:

A Prasanth Saraswati Nicola Relitti Margherita Brindisi Sandra Gemma Daniela Zisterer Stefania Butini Giuseppe Campiani

Drug Discov Today 2019 07 25;24(7):1370-1388. Epub 2019 May 25.

University of Siena, Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, via Aldo Moro 2, I-53100 Siena, Italy. Electronic address:

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July 2019

Dietary polyphenols rutin, taxifolin and quercetin related compounds target Leishmania amazonensis arginase.

Authors:

Edson Roberto da Silva Simone Brogi João Francisco Lucon-Júnior Giuseppe Campiani Sandra Gemma Claudia do Carmo Maquiaveli

Food Funct 2019 Jun;10(6):3172-3180

Departamento de Medicina Veterinária, Faculdade de Zootecnia e Engenharia de Alimentos, Universidade de São Paulo, Avenida Duque de Caxias Norte, 225, 13635-900 Pirassununga, SP, Brazil.

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June 2019

A light in the dark: state of the art and perspectives in optogenetics and optopharmacology for restoring vision.

Authors:

Giulia Chemi Margherita Brindisi Simone Brogi Nicola Relitti Stefania Butini Sandra Gemma Giuseppe Campiani

Future Med Chem 2019 03 25;11(5):463-487. Epub 2019 Mar 25.

Department of Biotechnology, Chemistry & Pharmacy, Department of Excellence 2018-2022, University of Siena, Via A. Moro 2, 53100 Siena, Italy.

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March 2019

Allosteric Modulation of Ionotropic Glutamate Receptors: An Outlook on New Therapeutic Approaches To Treat Central Nervous System Disorders.

Authors:

Simone Brogi Giuseppe Campiani Margherita Brindisi Stefania Butini

ACS Med Chem Lett 2019 Mar 23;10(3):228-236. Epub 2019 Jan 23.

Department of Biotechnology, Chemistry and Pharmacy, University of Siena, DoE Department of Excellence 2018-2022, via Aldo Moro 2, I-53100 Siena, Italy.

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March 2019

Synthesis, Molecular Modelling and Biological Studies of 3-hydroxypyrane- 4-one and 3-hydroxy-pyridine-4-one Derivatives as HIV-1 Integrase Inhibitors.

Authors:

Hajar Sirous Afshin Fassihi Simone Brogi Giuseppe Campiani Frauke Christ Zeger Debyser Sandra Gemma Stefania Butini Giulia Chemi Alessandro Grillo Rezvan Zabihollahi Mohammad R Aghasadeghi Lotfollah Saghaie Hamid R Memarian

Med Chem 2019 ;15(7):755-770

Department of Chemistry, Faculty of Sciences, University of Isfahan, 81746-73441 Isfahan, Iran.

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December 2019

Author Correction: The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity.

Authors:

Roberto Colangeli Massimo Pierucci Arcangelo Benigno Giuseppe Campiani Stefania Butini Giuseppe Di Giovanni

Sci Rep 2018 Dec 14;8(1):17977. Epub 2018 Dec 14.

Laboratory of Neurophysiology, Department of Physiology and Biochemistry, Faculty of Medicine and Surgery, University of Malta, Msida, Malta.

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December 2018

Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents.

Eur J Med Chem 2019 Jan 3;162:290-320. Epub 2018 Nov 3.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Department of Biotechnology, Chemistry and Pharmacy, DoE Department of Excellence 2018-2022, via Aldo Moro 2, I-53100, Siena, Italy; Istituto Toscano Tumori, University of Siena, via Aldo Moro 2, I-53100, Siena, Italy; Department of Pharmacy, University of Napoli Federico II, DoE Department of Excellence 2018-2022, Via D. Montesano 49, 80131, Napoli, Italy.

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January 2019

Cinnamic acids derived compounds with antileishmanial activity target Leishmania amazonensis arginase.

Authors:

Edson Roberto da Silva Simone Brogi Alessandro Grillo Giuseppe Campiani Sandra Gemma Paulo Cezar Vieira Claudia do Carmo Maquiaveli

Chem Biol Drug Des 2019 02 10;93(2):139-146. Epub 2018 Oct 10.

Universidade Anhembi Morumbi, São Paulo, Brazil.

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February 2019

Development of a Multiplexed Activity-Based Protein Profiling Assay to Evaluate Activity of Endocannabinoid Hydrolase Inhibitors.

Authors:

Antonius P A Janssen Daan van der Vliet Alexander T Bakker Ming Jiang Sebastian H Grimm Giuseppe Campiani Stefania Butini Mario van der Stelt

ACS Chem Biol 2018 09 12;13(9):2406-2413. Epub 2018 Sep 12.

Department of Molecular Physiology, LIC , Leiden University , Leiden , The Netherlands.

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September 2018

Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.

Eur J Med Chem 2018 Sep 31;157:127-138. Epub 2018 Jul 31.

European Research Centre for Drug Discovery and Development (NatSynDrugs) and Department of Biotechnology, Chemistry, and Pharmacy, Department of Excellence 2018-2022, University of Siena, via Aldo Moro 2, 53100, Siena, Italy.

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September 2018

Development of Potent Inhibitors of Fatty Acid Amide Hydrolase Useful for the Treatment of Neuropathic Pain.

Authors:

Margherita Brindisi Giuseppe Borrelli Simone Brogi Alessandro Grillo Samuele Maramai Marco Paolino Mascia Benedusi Alessandra Pecorelli Giuseppe Valacchi Lorenzo Di Cesare Mannelli Carla Ghelardini Marco Allarà Alessia Ligresti Patrizia Minetti Giuseppe Campiani Vincenzo di Marzo Stefania Butini Sandra Gemma

ChemMedChem 2018 10 30;13(19):2090-2103. Epub 2018 Aug 30.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Department of Biotechnology, Chemistry, and Pharmacy (DoE 2018-2020), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy.

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October 2018

iPSC-derived neurons profiling reveals GABAergic circuit disruption and acetylated α-tubulin defect which improves after iHDAC6 treatment in Rett syndrome.

Exp Cell Res 2018 07 4;368(2):225-235. Epub 2018 May 4.

Medical Genetics, University of Siena, Strada delle Scotte 4, 53100, Siena, Italy.

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July 2018

Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues.

Eur J Med Chem 2018 Apr 10;150:698-718. Epub 2018 Mar 10.

Department of Biotechnology, Chemistry and Pharmacy, Dipartimento di Eccellenza 2018-2022, University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.

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April 2018

Author Correction: The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity.

Authors:

Roberto Colangeli Massimo Pierucci Arcangelo Benigno Giuseppe Campiani Stefania Butini Giuseppe Di Giovanni

Sci Rep 2018 Mar 12;8(1):4648. Epub 2018 Mar 12.

Laboratory of Neurophysiology, Department of Physiology and Biochemistry, Faculty of Medicine and Surgery, University of Malta, Msida, Malta.

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March 2018

( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.

Authors:

Simone Brogi Margherita Brindisi Stefania Butini Giridhar U Kshirsagar Samuele Maramai Giulia Chemi Sandra Gemma Giuseppe Campiani Ettore Novellino Paolo Fiorenzani Jessica Pinassi Anna Maria Aloisi Mikko Gynther Raminta Venskutonytė Liwei Han Karla Frydenvang Jette Sandholm Kastrup Darryl S Pickering

J Med Chem 2018 03 26;61(5):2124-2130. Epub 2018 Feb 26.

Department of Drug Design and Pharmacology , University of Copenhagen , Jagtvej 162 , DK-2100 Copenhagen , Denmark.

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March 2018

Development of Potent Inhibitors of the Mycobacterium tuberculosis Virulence Factor Zmp1 and Evaluation of Their Effect on Mycobacterial Survival inside Macrophages.

ChemMedChem 2018 03 14;13(5):422-430. Epub 2018 Feb 14.

European Research Centre for Drug Discovery and Development - NatSynDrugs - and Department of Biotechnology, Chemistry, and Pharmacy, University of Siena, via Aldo Moro 1, 53100, Siena, Italy.

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March 2018

Activation of the Wnt Pathway by Small Peptides: Rational Design, Synthesis and Biological Evaluation.

Authors:

Simone Brogi Samuele Maramai Margherita Brindisi Giulia Chemi Valentina Porcari Claudio Corallo Luigi Gennari Ettore Novellino Anna Ramunno Stefania Butini Giuseppe Campiani Sandra Gemma

ChemMedChem 2017 12 29;12(24):2074-2085. Epub 2017 Nov 29.

European Research Centre for Drug Discovery and Development, NatSynDrugs and Department of Biotechnology, Chemistry, and Pharmacy, University of Siena, via Aldo Moro 2, 53100, Siena, Italy.

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December 2017

The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity.

Authors:

Roberto Colangeli Massimo Pierucci Arcangelo Benigno Giuseppe Campiani Stefania Butini Giuseppe Di Giovanni

Sci Rep 2017 09 11;7(1):11152. Epub 2017 Sep 11.

Laboratory of Neurophysiology, Department of Physiology and Biochemistry, Faculty of Medicine and Surgery, University of Malta, Msida, Malta.

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September 2017

First dual AK/GSK-3β inhibitors endowed with antioxidant properties as multifunctional, potential neuroprotective agents.

Authors:

Simone Brogi Anna Ramunno Lida Savi Giulia Chemi Gloria Alfano Alessandra Pecorelli Erika Pambianchi Paola Galatello Giulia Compagnoni Federico Focher Giuseppe Biamonti Giuseppe Valacchi Stefania Butini Sandra Gemma Giuseppe Campiani Margherita Brindisi

Eur J Med Chem 2017 Sep 9;138:438-457. Epub 2017 Jun 9.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Department of Biotechnology, Chemistry, and Pharmacy, Università degli Studi di Siena via Aldo Moro 2, 53100 Siena, Italy.

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September 2017

Computational Tool for Fast Evaluation of ERG K Channel Affinity.

Authors:

Giulia Chemi Sandra Gemma Giuseppe Campiani Simone Brogi Stefania Butini Margherita Brindisi

Front Chem 2017 23;5. Epub 2017 Feb 23.

European Research Centre for Drug Discovery (NatSynDrugs), University of SienaSiena, Italy.

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February 2017

Structural characterization of Giardia duodenalis thioredoxin reductase (gTrxR) and computational analysis of its interaction with NBDHEX.

Authors:

Simone Brogi Annarita Fiorillo Giulia Chemi Stefania Butini Marco Lalle Andrea Ilari Sandra Gemma Giuseppe Campiani

Eur J Med Chem 2017 Jul 24;135:479-490. Epub 2017 Apr 24.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Department of Biotechnology, Chemistry, and Pharmacy, Università di Siena via Aldo Moro 2, 53100 Siena, Italy.

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July 2017

Identification of novel fluorescent probes preventing PrP replication in prion diseases.

Authors:

Ludovica Zaccagnini Simone Brogi Margherita Brindisi Sandra Gemma Giulia Chemi Giuseppe Legname Giuseppe Campiani Stefania Butini

Eur J Med Chem 2017 Feb 1;127:859-873. Epub 2016 Nov 1.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università degli Studi di Siena, via Aldo Moro 2, 53100 Siena, Italy; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, via Aldo Moro 2, 53100 Siena, Italy.

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February 2017

Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases.

Authors:

Samuele Maramai Sandra Gemma Simone Brogi Giuseppe Campiani Stefania Butini Holger Stark Margherita Brindisi

Front Neurosci 2016 5;10:451. Epub 2016 Oct 5.

European Research Centre for Drug Discovery and Development and Department of Biotechnology, Chemistry and Pharmacy, University of Siena Siena, Italy.

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October 2016

Phenylpyrrole-based HDAC inhibitors: synthesis, molecular modeling and biological studies.

Authors:

Margherita Brindisi Caterina Cavella Simone Brogi Angela Nebbioso Johanna Senger Samuele Maramai Alfonso Ciotta Concetta Iside Stefania Butini Stefania Lamponi Ettore Novellino Lucia Altucci Manfred Jung Giuseppe Campiani Sandra Gemma

Future Med Chem 2016 09 24;8(13):1573-87. Epub 2016 Aug 24.

European Research Centre for Drug Discovery & Development (NatSynDrugs), University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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September 2016

Involvement of AMP-activated protein kinase in mediating pyrrolo-1,5-benzoxazepine-induced apoptosis in neuroblastoma cells.

Authors:

Jennifer C Lennon Stefania Butini Giuseppe Campiani Anne O'Meara D Clive Williams Daniela M Zisterer

Invest New Drugs 2016 10 22;34(5):663-76. Epub 2016 Jun 22.

School of Biochemistry and Immunology, Trinity Biomedical Sciences Institute, Trinity College Dublin, 152-160 Pearse Street, Dublin 2, Ireland.

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October 2016

The pyrrolo-1,5-benzoxazepine, PBOX-15, enhances TRAIL‑induced apoptosis by upregulation of DR5 and downregulation of core cell survival proteins in acute lymphoblastic leukaemia cells.

Authors:

Seema-Maria Nathwani Lisa M Greene Stefania Butini Giuseppe Campiani D Clive Williams Afshin Samali Eva Szegezdi Daniela M Zisterer

Int J Oncol 2016 Jul 12;49(1):74-88. Epub 2016 May 12.

School of Biochemistry and Immunology, Trinity Biomedical Sciences Institute, Trinity College Dublin, Dublin 2, Ireland.

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July 2016

Development of novel cyclic peptides as pro-apoptotic agents.

Eur J Med Chem 2016 Jul 5;117:301-20. Epub 2016 Apr 5.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Siena University, via Aldo Moro 2, I-53100 Siena, Italy; Istituto Toscano Tumori, Siena University, via Aldo Moro 2, I-53100 Siena, Italy.

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July 2016

Targeting clinically-relevant metallo-β-lactamases: from high-throughput docking to broad-spectrum inhibitors.

Authors:

Margherita Brindisi Simone Brogi Simone Giovani Sandra Gemma Stefania Lamponi Filomena De Luca Ettore Novellino Giuseppe Campiani Jean-Denis Docquier Stefania Butini

J Enzyme Inhib Med Chem 2016 28;31(sup1):98-109. Epub 2016 Apr 28.

a European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena , Siena , Italy.

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February 2017

Verbascoside Inhibits Promastigote Growth and Arginase Activity of Leishmania amazonensis.

Authors:

Claudia C Maquiaveli João F Lucon-Júnior Simone Brogi Giuseppe Campiani Sandra Gemma Paulo C Vieira Edson R Silva

J Nat Prod 2016 05 20;79(5):1459-63. Epub 2016 Apr 20.

Department of Veterinary Medicine, Universidade de São Paulo , Avenida Duque de Caxias Norte, 225, 13635-900 Pirassununga, SP, Brazil.

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May 2016

Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain.

J Med Chem 2016 03 7;59(6):2612-32. Epub 2016 Mar 7.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena , via Aldo Moro 2, I-53100 Siena, Italy.

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March 2016

The novel pyrrolo-1,5-benzoxazepine, PBOX-15, synergistically enhances the apoptotic efficacy of imatinib in gastrointestinal stromal tumours; suggested mechanism of action of PBOX-15.

Authors:

Paula Kinsella Lisa M Greene Sandra A Bright Jade K Pollock Stefania Butini Giuseppe Campiani Sebastian Bauer D Clive Williams Daniela M Zisterer

Invest New Drugs 2016 Apr 17;34(2):159-67. Epub 2016 Feb 17.

School of Biochemistry and Immunology, Trinity Biomedical Sciences Institute, Trinity College Dublin, 152-160 Pearse Street, Dublin 2, Ireland.

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April 2016

In silico study of subtilisin-like protease 1 (SUB1) from different Plasmodium species in complex with peptidyl-difluorostatones and characterization of potent pan-SUB1 inhibitors.

Authors:

Simone Brogi Simone Giovani Margherita Brindisi Sandra Gemma Ettore Novellino Giuseppe Campiani Michael J Blackman Stefania Butini

J Mol Graph Model 2016 Mar 19;64:121-130. Epub 2016 Jan 19.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, via Aldo Moro 2, 53100, Siena, Italy; Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, via Aldo Moro 2, 53100, Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.

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March 2016

Multitarget compounds bearing tacrine- and donepezil-like structural and functional motifs for the potential treatment of Alzheimer's disease.

Authors:

Lhassane Ismaili Bernard Refouvelet Mohamed Benchekroun Simone Brogi Margherita Brindisi Sandra Gemma Giuseppe Campiani Slavica Filipic Danica Agbaba Gerard Esteban Mercedes Unzeta Katarina Nikolic Stefania Butini José Marco-Contelles

Prog Neurobiol 2017 04 18;151:4-34. Epub 2016 Jan 18.

Laboratory of Medicinal Chemistry (IQOG, CSIC), C/ Juan de la Cierva 3, 28006 Madrid, Spain. Electronic address:

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April 2017

Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.

Authors:

Ming-Yu Wu Gerard Esteban Simone Brogi Masahi Shionoya Li Wang Giuseppe Campiani Mercedes Unzeta Tsutomu Inokuchi Stefania Butini Jose Marco-Contelles

Eur J Med Chem 2016 Oct 9;121:864-879. Epub 2015 Oct 9.

Laboratory of Medicinal Chemistry (IQOG, CSIC), C/Juan de la Cierva 3, 28006 Madrid, Spain. Electronic address:

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October 2016

Exploring clotrimazole-based pharmacophore: 3D-QSAR studies and synthesis of novel antiplasmodial agents.

Authors:

Simone Brogi Margherita Brindisi Bhupendra P Joshi Salvatore Sanna Coccone Silvia Parapini Nicoletta Basilico Ettore Novellino Giuseppe Campiani Sandra Gemma Stefania Butini

Bioorg Med Chem Lett 2015 Nov 5;25(22):5412-8. Epub 2015 Sep 5.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università degli Studi di Siena, via Aldo Moro 2, 53100 Siena, Italy; Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, via Aldo Moro 2, 53100 Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.

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November 2015

Antitumor effect of pyrrolo-1,5-benzoxazepine-15 and its synergistic effect with Oxaliplatin and 5-FU in colorectal cancer cells.

Authors:

Donatella Fiore Maria Chiara Proto Simona Pisanti Paola Picardi Antonio Christian Pagano Zottola Stefania Butini Sandra Gemma Alice Casagni Chiara Laezza Mario Vitale Alessia Ligresti Vincenzo Di Marzo Daniela M Zisterer Seema Nathwani D Clive Williams Giuseppe Campiani Patrizia Gazzerro Maurizio Bifulco

Cancer Biol Ther 2016 08;17(8):849-58

d Department of Medicine and Surgery , University of Salerno , Baronissi (SA) , Italy.

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August 2016

Endocannabinoid Modulation of Predator Stress-Induced Long-Term Anxiety in Rats.

Authors:

James Lim Miki Igarashi Kwang-Mook Jung Stefania Butini Giuseppe Campiani Daniele Piomelli

Neuropsychopharmacology 2016 Apr 11;41(5):1329-39. Epub 2015 Sep 11.

Department of Anatomy and Neurobiology, University of California, Irvine, CA, USA.

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April 2016

Unconventional Knoevenagel-type indoles: Synthesis and cell-based studies for the identification of pro-apoptotic agents.

Authors:

Andrea Spallarossa Chiara Caneva Matteo Caviglia Silvana Alfei Stefania Butini Giuseppe Campiani Sandra Gemma Margherita Brindisi Daniela M Zisterer Sandra A Bright Clive D Williams Emmanuele Crespan Giovanni Maga Giuseppina Sanna Ilenia Delogu Gabriella Collu Roberta Loddo

Eur J Med Chem 2015 Sep 8;102:648-60. Epub 2015 Aug 8.

Dipartimento di Scienze Biomediche, Sezione di Microbiologia e Virologia, Università di Cagliari, Cittadella Universitaria, s.p. 8, Km 0.700, I-09042 Monserrato, Cagliari, Italy.

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September 2015

Site-directed Mutagenesis of Key Residues Unveiled a Novel Allosteric Site on Human Adenosine Kinase for Pyrrolobenzoxa(thia)zepinone Non-Nucleoside Inhibitors.

Authors:

Lida Savi Margherita Brindisi Gloria Alfano Stefania Butini Valeria La Pietra Ettore Novellino Luciana Marinelli Andrea Lossani Federico Focher Caterina Cavella Giuseppe Campiani Sandra Gemma

Chem Biol Drug Des 2016 Jan 18;87(1):112-20. Epub 2015 Sep 18.

Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, via Aldo Moro 2, 53100, Siena, Italy.

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January 2016

Induction of apoptosis in oral squamous carcinoma cells by pyrrolo-1,5-benzoxazepines.

Authors:

Kate O'Callaghan Eleonora Palagano Stefania Butini Giuseppe Campiani D Clive Williams Daniela M Zisterer Jeff O'Sullivan

Mol Med Rep 2015 Sep 25;12(3):3748-3754. Epub 2015 May 25.

School of Dental Science, Trinity College Dublin, Dublin 2, Ireland.

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September 2015

Structure-based discovery of the first non-covalent inhibitors of Leishmania major tryparedoxin peroxidase by high throughput docking.

Authors:

Margherita Brindisi Simone Brogi Nicola Relitti Alessandra Vallone Stefania Butini Sandra Gemma Ettore Novellino Gianni Colotti Gabriella Angiulli Francesco Di Chiaro Annarita Fiorillo Andrea Ilari Giuseppe Campiani

Sci Rep 2015 May 7;5:9705. Epub 2015 May 7.

1] European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, via Aldo Moro 2, 53100, Siena [2] Dip. di Biotecnologie, Chimica e Farmacia, University of Siena, via Aldo Moro 2, 53100, Siena, Italy.

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May 2015

Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.

Authors:

Margherita Brindisi Stefania Butini Silvia Franceschini Simone Brogi Francesco Trotta Sindu Ros Alfredo Cagnotto Mario Salmona Alice Casagni Marco Andreassi Simona Saponara Beatrice Gorelli Pia Weikop Jens D Mikkelsen Jorgen Scheel-Kruger Karin Sandager-Nielsen Ettore Novellino Giuseppe Campiani Sandra Gemma

J Med Chem 2014 Nov 7;57(22):9578-97. Epub 2014 Nov 7.

European Research Centre for Drug Discovery and Development, and ‡Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena , via Aldo Moro 2, 53100 Siena, Italy.

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November 2014

Disease-modifying anti-Alzheimer's drugs: inhibitors of human cholinesterases interfering with β-amyloid aggregation.

Authors:

Simone Brogi Stefania Butini Samuele Maramai Raffaella Colombo Laura Verga Cristina Lanni Ersilia De Lorenzi Stefania Lamponi Marco Andreassi Manuela Bartolini Vincenza Andrisano Ettore Novellino Giuseppe Campiani Margherita Brindisi Sandra Gemma

CNS Neurosci Ther 2014 Jul;20(7):624-32

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Siena, Italy; Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, Siena, Italy.

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July 2014

Rational design of the first difluorostatone-based PfSUB1 inhibitors.

Authors:

Simone Giovani Maria Penzo Simone Brogi Margherita Brindisi Sandra Gemma Ettore Novellino Luisa Savini Michael J Blackman Giuseppe Campiani Stefania Butini

Bioorg Med Chem Lett 2014 Aug 23;24(15):3582-6. Epub 2014 May 23.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, via Aldo Moro 2, 53100 Siena, Italy; Dip. di Biotecnologie, Chimica e Farmacia, University of Siena, via Aldo Moro 2, 53100 Siena, Italy; Centro Interuniversitario di Ricerche sulla Malaria (CIRM), University of Perugia, Perugia, Italy.

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August 2014

Multifunctional cholinesterase and amyloid Beta fibrillization modulators. Synthesis and biological investigation.

Authors:

Stefania Butini Margherita Brindisi Simone Brogi Samuele Maramai Egeria Guarino Alessandro Panico Ashima Saxena Ved Chauhan Raffaella Colombo Laura Verga Ersilia De Lorenzi Manuela Bartolini Vincenza Andrisano Ettore Novellino Giuseppe Campiani Sandra Gemma

ACS Med Chem Lett 2013 Dec 6;4(12):1178-82. Epub 2013 Oct 6.

European Research Centre for Drug Discovery and Development-NatSynDrugs and Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena , via Aldo Moro 2, 53100 Siena, Italy ; European Research Centre for Drug Discovery and Development-NatSynDrugs and Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena , via Aldo Moro 2, 53100 Siena, Italy.

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December 2013

Synthesis and structure-activity relationship studies in serotonin 5-HT4 receptor ligands based on a benzo[de][2,6]naphthridine scaffold.

Authors:

Federica Castriconi Marco Paolino Germano Giuliani Maurizio Anzini Giuseppe Campiani Laura Mennuni Chiara Sabatini Marco Lanza Gianfranco Caselli Francesca De Rienzo Maria Cristina Menziani Maria Sbraccia Paola Molinari Tommaso Costa Andrea Cappelli

Eur J Med Chem 2014 Jul 5;82:36-46. Epub 2014 May 5.

Dipartimento di Biotecnologie, Chimica e Farmacia and European Research Centre for Drug Discovery and Development, Università degli Studi di Siena, Via A. Moro 2, 53100 Siena, Italy. Electronic address:

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July 2014

The novel pyrrolo-1,5-benzoxazepine, PBOX-6, synergistically enhances the apoptotic effects of carboplatin in drug sensitive and multidrug resistant neuroblastoma cells.

Authors:

Jennifer C Lennon Sandra A Bright Eilis Carroll Stefania Butini Giuseppe Campiani Anne O'Meara D Clive Williams Daniela M Zisterer

Biochem Pharmacol 2014 Feb 6;87(4):611-24. Epub 2014 Jan 6.

School of Biochemistry and Immunology, Trinity Biomedical Sciences Institute, Trinity College Dublin, 152-160 Pearse Street, Dublin 2, Ireland. Electronic address:

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February 2014

A stereoselective approach to peptidomimetic BACE1 inhibitors.

Authors:

Stefania Butini Emanuele Gabellieri Margherita Brindisi Simone Giovani Samuele Maramai Giridhar Kshirsagar Egeria Guarino Simone Brogi Valeria La Pietra Mariateresa Giustiniano Luciana Marinelli Ettore Novellino Giuseppe Campiani Andrea Cappelli Sandra Gemma

Eur J Med Chem 2013 6;70:233-47. Epub 2013 Oct 6.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, via Aldo Moro 2, 53100 Siena, Italy; Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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September 2014

HCV-targeted antivirals: current status and future challenges.

Authors:

Sandra Gemma Simone Brogi Ettore Novellino Giuseppe Campiani Giovanni Maga Margherita Brindisi Stefania Butini

Curr Pharm Des 2014 ;20(21):3445-64

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università di Siena, via Aldo Moro 2, 53100, Siena (Italy).

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March 2015

The structural evolution of β-secretase inhibitors: a focus on the development of small-molecule inhibitors.

Authors:

Stefania Butini Simone Brogi Ettore Novellino Giuseppe Campiani Arun K Ghosh Margherita Brindisi Sandra Gemma

Curr Top Med Chem 2013 ;13(15):1787-807

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via Aldo Moro, 2, 53100 Siena, Italy.

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March 2014

PBOX-15 induces apoptosis and improves the efficacy of oxaliplatin in human colorectal cancer cell lines.

Authors:

Giuseppina Gangemi Patrizia Gazzerro Donatella Fiore Maria Chiara Proto Stefania Butini Sandra Gemma Alice Casagni Chiara Laezza Mario Vitale Alessia Ligresti Vincenzo Di Marzo Daniela M Zisterer Seema Nathwani D Clive Williams Giuseppe Campiani Maurizio Bifulco

Eur J Pharmacol 2013 Aug 16;714(1-3):379-87. Epub 2013 Jul 16.

Department of Pharmacy, University of Salerno, 84084 Fisciano, SA, Italy.

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August 2013

Inhibition of late-stage autophagy synergistically enhances pyrrolo-1,5-benzoxazepine-6-induced apoptotic cell death in human colon cancer cells.

Authors:

Lisa M Greene Derek P Nolan Daniel Regan-Komito Giuseppe Campiani D Clive Williams Daniela M Zisterer

Int J Oncol 2013 Sep 25;43(3):927-35. Epub 2013 Jun 25.

School of Biochemistry and Immunology, Trinity Biomedical Sciences Institute, Trinity College Dublin, Dublin 2, Ireland.

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September 2013

Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.

Authors:

Andrea Cappelli Monica Manini Salvatore Valenti Federica Castriconi Germano Giuliani Maurizio Anzini Simone Brogi Stefania Butini Sandra Gemma Giuseppe Campiani Gianluca Giorgi Laura Mennuni Marco Lanza Antonio Giordani Gianfranco Caselli Ornella Letari Francesco Makovec

Eur J Med Chem 2013 May 8;63:85-94. Epub 2013 Feb 8.

Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Università degli Studi di Siena, Via A. Moro, 53100 Siena, Italy.

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May 2013

Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties.

Authors:

Stefania Butini Sandra Gemma Margherita Brindisi Samuele Maramai Patrizia Minetti Diana Celona Raffaella Napolitano Franco Borsini Walter Cabri Filomena Fezza Lucio Merlini Sabrina Dallavalle Giuseppe Campiani Mauro Maccarrone

Bioorg Med Chem Lett 2013 Jan 22;23(2):492-5. Epub 2012 Nov 22.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università degli Studi di Siena, Via Aldo Moro, 53100 Siena, Italy.

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January 2013

Novel peptidomimetics as BACE-1 inhibitors: synthesis, molecular modeling, and biological studies.

Authors:

Stefania Butini Emanuele Gabellieri Margherita Brindisi Alice Casagni Egeria Guarino Paul B Huleatt Nicola Relitti Valeria La Pietra Luciana Marinelli Mariateresa Giustiniano Ettore Novellino Giuseppe Campiani Sandra Gemma

Bioorg Med Chem Lett 2013 Jan 14;23(1):85-9. Epub 2012 Nov 14.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università degli Studi di Siena, Via Aldo Moro 2, 53100 Siena, Italy.

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January 2013

Mimicking the intramolecular hydrogen bond: synthesis, biological evaluation, and molecular modeling of benzoxazines and quinazolines as potential antimalarial agents.

J Med Chem 2012 Dec 21;55(23):10387-404. Epub 2012 Nov 21.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Dipartimento di Neuroscienze, University of Siena, Via Aldo Moro, 53100 Siena, Italy.

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December 2012

The microtubule targeting agent PBOX-15 inhibits integrin-mediated cell adhesion and induces apoptosis in acute lymphoblastic leukaemia cells.

Authors:

Joanne Lysaght Navin K Verma Elaina N Maginn Jacqueline M Ryan Giuseppe Campiani Daniela M Zisterer D Clive Williams Paul V Browne Mark P Lawler Anthony M McElligott

Int J Oncol 2013 Jan 6;42(1):239-46. Epub 2012 Nov 6.

Department of Haematology, Trinity College, Dublin, Ireland.

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January 2013

A straightforward approach for engineering efficacy and selectivity at GPCRs.

Authors:

Stefania Butini Sandra Gemma Giuseppe Campiani

J Med Chem 2012 Aug 18;55(15):6687-8. Epub 2012 Jul 18.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università degli Studi di Siena , Via Aldo Moro 2, 53100 Siena, Italy.

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August 2012

Quinolylhydrazones as novel inhibitors of Plasmodium falciparum serine protease PfSUB1.

Authors:

Sandra Gemma Simone Giovani Margherita Brindisi Pierangela Tripaldi Simone Brogi Luisa Savini Isabella Fiorini Ettore Novellino Stefania Butini Giuseppe Campiani Maria Penzo Michael J Blackman

Bioorg Med Chem Lett 2012 Aug 23;22(16):5317-21. Epub 2012 Jun 23.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, Via A. Moro, 53100 Siena, Italy.

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August 2012

Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling.

J Med Chem 2012 Aug 27;55(15):6948-67. Epub 2012 Jul 27.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università di Siena , Via A. Moro, 53100 Siena, Italy.

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August 2012

Discovery of potent inhibitors of human and mouse fatty acid amide hydrolases.

Authors:

Stefania Butini Margherita Brindisi Sandra Gemma Patrizia Minetti Walter Cabri Grazia Gallo Silvia Vincenti Emanuela Talamonti Franco Borsini Antonio Caprioli Maria Antonietta Stasi Stefano Di Serio Sindu Ros Giuseppe Borrelli Samuele Maramai Filomena Fezza Giuseppe Campiani Mauro Maccarrone

J Med Chem 2012 Aug 26;55(15):6898-915. Epub 2012 Jul 26.

European Research Centre for Drug Discovery and Development (NatSynDrugs), Università degli Studi di Siena , Via Aldo Moro 2, 53100 Siena, Italy.

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August 2012

Broad inhibition of plasmodium falciparum cytoadherence by (+)-epigallocatechin gallate.

Authors:

Pradeep R Patil Sandra Gemma Giuseppe Campiani Alister G Craig

Malar J 2011 Dec 1;10:348. Epub 2011 Dec 1.

European Research Centre for Drug Discovery and Development, Department of Pharmaceutical and Applied Chemistry, University of Siena, Italy.

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December 2011

The Ca2+-ATPase (SERCA1) is inhibited by 4-aminoquinoline derivatives through interference with catalytic activation by Ca2+, whereas the ATPase E2 state remains functional.

Authors:

Gianluca Bartolommei Francesco Tadini-Buoninsegni Maria Rosa Moncelli Sandra Gemma Caterina Camodeca Stefania Butini Giuseppe Campiani David Lewis Giuseppe Inesi

J Biol Chem 2011 Nov 13;286(44):38383-9. Epub 2011 Sep 13.

Department of Chemistry Ugo Schiff, University of Florence, 50019 Sesto Fiorentino, Italy.

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November 2011

Synthesis and antiplasmodial activity of bicyclic dioxanes as simplified dihydroplakortin analogues.

Authors:

Sandra Gemma Sanil Kunjir Salvatore Sanna Coccone Margherita Brindisi Vittoria Moretti Simone Brogi Ettore Novellino Nicoletta Basilico Silvia Parapini Donatella Taramelli Giuseppe Campiani Stefania Butini

J Med Chem 2011 Aug 29;54(16):5949-53. Epub 2011 Jul 29.

European Research Centre for Drug Discovery and Development (NatSynDrugs), 53100 Siena, Italy.

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August 2011

Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants.

Authors:

Stefania Butini Sandra Gemma Margherita Brindisi Giuseppe Borrelli Isabella Fiorini Alberta Samuele Aristotele Karytinos Marcella Facchini Andrea Lossani Samantha Zanoli Giuseppe Campiani Ettore Novellino Federico Focher Giovanni Maga

Bioorg Med Chem Lett 2011 Jul 14;21(13):3935-8. Epub 2011 May 14.

European Research Centre for Drug Discovery and Development (NatSynDrugs), via Aldo Moro, 2-Università di Siena, 53100 Siena, Italy.

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July 2011

Pyrroloquinoxaline hydrazones as fluorescent probes for amyloid fibrils.

Authors:

Sandra Gemma Laura Colombo Gianluigi Forloni Luisa Savini Claudia Fracasso Silvio Caccia Mario Salmona Margherita Brindisi Bhupendra P Joshi Pierangela Tripaldi Gianluca Giorgi Orazio Taglialatela-Scafati Ettore Novellino Isabella Fiorini Giuseppe Campiani Stefania Butini

Org Biomol Chem 2011 Jul 1;9(14):5137-48. Epub 2011 Jun 1.

European Research Centre for Drug Discovery and Development (NatSynDrugs), University of Siena, via Aldo Moro, 53100, Siena, Italy.

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July 2011

Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.

Authors:

Raminta Venskutonyte Stefania Butini Salvatore Sanna Coccone Sandra Gemma Margherita Brindisi Vinod Kumar Egeria Guarino Samuele Maramai Salvatore Valenti Ahmad Amir Elena Antón Valadés Karla Frydenvang Jette S Kastrup Ettore Novellino Giuseppe Campiani Darryl S Pickering

J Med Chem 2011 Jul 13;54(13):4793-805. Epub 2011 Jun 13.

Department of Pharmacology and Pharmacotherapy, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, Denmark.

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July 2011

Non-nucleoside inhibitors of human adenosine kinase: synthesis, molecular modeling, and biological studies.

J Med Chem 2011 Mar 14;54(5):1401-20. Epub 2011 Feb 14.

European Research Centre for Drug Discovery and Development, NatSynDrugs, Università di Siena, 53100 Siena, Italy.

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March 2011

Novel microtubule-targeting agents, pyrrolo-1,5-benzoxazepines, induce cell cycle arrest and apoptosis in prostate cancer cells.

Authors:

Seema-Maria Nathwani Suzanne M Cloonan Maeve Stronach Giuseppe Campiani Mark Lawler D Clive Williams Daniela M Zisterer

Oncol Rep 2010 Dec;24(6):1499-507

School of Biochemistry and Immunology, Trinity College, Dublin 2, Ireland.

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December 2010

Discovery of potent nucleotide-mimicking competitive inhibitors of hepatitis C virus NS3 helicase.

Authors:

Sandra Gemma Stefania Butini Giuseppe Campiani Margherita Brindisi Samantha Zanoli Maria Pia Romano Pierangela Tripaldi Luisa Savini Isabella Fiorini Giuseppe Borrelli Ettore Novellino Giovanni Maga

Bioorg Med Chem Lett 2011 May 6;21(9):2776-9. Epub 2010 Sep 6.

European Research Centre for Drug Discovery and Development, Università di Siena, via Aldo Moro, 53100 Siena, Italy.

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May 2011

Malaria chemotherapy: recent advances in drug development.

Authors:

Sandra Gemma Valter Travagli Luisa Savini Ettore Novellino Giuseppe Campiani Stefania Butini

Recent Pat Antiinfect Drug Discov 2010 Nov;5(3):195-225

Department of Pharmaceutical and Applied Chemistry, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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November 2010

Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.

Authors:

Stefania Butini Giuseppe Campiani Silvia Franceschini Francesco Trotta Vinod Kumar Egeria Guarino Giuseppe Borrelli Isabella Fiorini Ettore Novellino Caterina Fattorusso Marco Persico Nausicaa Orteca Karin Sandager-Nielsen Thomas Amos Jacobsen Kim Madsen Jorgen Scheel-Kruger Sandra Gemma

J Med Chem 2010 Jun;53(12):4803-7

European Research Centre for Drug Discovery and Development, Universita di Siena, 53100 Siena, Italy.

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June 2010

Sequential treatment with flavopiridol synergistically enhances pyrrolo-1,5-benzoxazepine-induced apoptosis in human chronic myeloid leukaemia cells including those resistant to imatinib treatment.

Authors:

Sandra A Bright Giuseppe Campiani Michael W Deininger Mark Lawler D Clive Williams Daniela M Zisterer

Biochem Pharmacol 2010 Jul 3;80(1):31-8. Epub 2010 Mar 3.

School of Biochemistry and Immunology, Trinity College, Dublin 2, Ireland.

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July 2010

Synthesis of dihydroplakortin, 6-epi-dihydroplakortin, and their C10-desethyl analogues.

Authors:

Sandra Gemma Emanuele Gabellieri Salvatore Sanna Coccone Francesc Martí Orazio Taglialatela-Scafati Ettore Novellino Giuseppe Campiani Stefania Butini

J Org Chem 2010 Apr;75(7):2333-40

Dipartimento Farmaco Chimico Tecnologico (DFCT), University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

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April 2010

The interactions of the 5-HT3 receptor with quipazine-like arylpiperazine ligands: the journey track at the end of the first decade of the third millennium.

Authors:

Andrea Cappelli Stefania Butini Antonella Brizzi Sandra Gemma Salvatore Valenti Germano Giuliani Maurizio Anzini Laura Mennuni Giuseppe Campiani Vittorio Brizzi Salvatore Vomero

Curr Top Med Chem 2010 ;10(5):504-26

Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Università di Siena, Via A. Moro, 53100 Siena, Italy.

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September 2010