Dr. Giuseppe Giannini, PhD - Alfasigma S.p.A. - Head of Medicinal Chemistry - Project Leader

Dr. Giuseppe Giannini

PhD

Alfasigma S.p.A.

Head of Medicinal Chemistry - Project Leader

Pomezia, Roma | Italy

Main Specialties: Chemistry

Additional Specialties: Medicinal Chemistry

ORCID logohttps://orcid.org/0000-0002-7127-985X

Dr. Giuseppe Giannini, PhD - Alfasigma S.p.A. - Head of Medicinal Chemistry - Project Leader

Dr. Giuseppe Giannini

PhD

Introduction

Primary Affiliation: Alfasigma S.p.A. - Pomezia, Roma , Italy

Specialties:

Additional Specialties:

Research Interests:


View Dr. Giuseppe Giannini’s Resume / CV

Education

Feb 1988
University of Bari
Master's Degree in Pharmacy
Dec 1986
University of Bari
Master's Degree in Chemistry
Graduated summa cum laude

Experience

Jan 2014
Project Leader (Leadiant Bioscience S.A. - former STRCH)
Medicinal Chemist (project coordinator)
Jan 2014 - Apr 2017
Feb 1995
Senior Scientist Alfasigma SpA, former Sigma-Tau)
Medicinal Chemist (Head)
to date
Jun 1989
Researcher - Senior Researcher (Menarini Ricerche)
Medicinal Chemist
Jun 1989 - Jan 1995

Publications

75Publications

893Reads

993Profile Views

Growth inhibition of human ovarian carcinoma by a novel AvidinOX-anchored biotinylated camptothecin derivative.

Bioorg Med Chem Lett 2018 Nov 15;28(20):3312-3314. Epub 2018 Sep 15.

Biotechnology, Research & Development, Alfasigma SpA, 00071 Pomezia (RM), Italy. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2018.09.017DOI Listing
November 2018
10 Reads
2.420 Impact Factor

Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo.

Eur J Med Chem 2018 Sep 27;157:368-379. Epub 2018 Jul 27.

Research & Development, Alfasigma SpA, via Pontina, Km 30.400, I-00040, Pomezia, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2018.07.053DOI Listing
September 2018
5 Reads
3.447 Impact Factor

Synthesis of Bromoundecyl Resorc[4]arenes and Applications of the Cone Stereoisomer as Selector for Liquid Chromatography.

J Org Chem 2018 Aug 11;83(15):7683-7693. Epub 2018 Jun 11.

Dipartimento di Chimica e Tecnologie del Farmaco , Sapienza Università di Roma , P.le A. Moro 5 , 00185 Roma , Italy.

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http://dx.doi.org/10.1021/acs.joc.8b00488DOI Listing
August 2018
9 Reads
4.721 Impact Factor

Novel Benzazole Derivatives Endowed with Potent Antiheparanase

J. Med. Chem. 2018, 61, 6918−6936

J.Med.Chem.

Heparanase is the sole mammalian enzyme capable of cleaving glycosaminoglycan heparan sulfate side chains of heparan sulfate proteoglycans. Its altered activity is intimately associated with tumor growth, angiogenesis, and metastasis. Thus, its implication in cancer progression makes it an attractive target in anticancer therapy. Herein, we describe the design, synthesis, and biological evaluation of new benzazoles as heparanase inhibitors. Most of the designed derivatives were active at micromolar or submicromolar concentration, and the most promising compounds are fluorinated and/or amino acids derivatives 13a, 14d, and 15 that showed IC50 0.16−0.82 μM. Molecular docking studies were performed to rationalize their interaction with the enzyme catalytic site. Importantly, invasion assay confirmed the antimetastatic potential of compounds 14d and 15. Consistently with its ability to inhibit heparanase, compound 15 proved to decrease expression of genes encoding for proangiogenic factors such as MMP-9, VEGF, and FGFs in tumor cells.

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July 2018
3 Reads

Roneparstat and Heparanase Inhibition: A New Tool for Cancer Treatment.

Pharmacol Clin Toxicol 5(2):1071

Journal of Pharmacology & Clinical Toxicology

Heparanase inhibition represents a new and interesting target for addressing cancer as well as other inflammatory-based diseases. This target is still largely underexploited. Heparanase activity releases from the extracellular matrix (ECM) and tumor microenvironment a multitude of heparan sulphate (HS)-bound growth factors, cytokines, chemokines, and enzymes that affect cells and tissue functions such as inflammation, wound healing and tumor invasion. A pro-metastatic and pro-angiogenic role for this enzyme has been widely demonstrated in many primary human tumors since high levels of heparanase correlate with lymph node and distant metastasis, elevated microvessel density and reduced survival of cancer patients. Heparanase is up regulated in many human hematologic and solid tumors. Two HS mimetics, PG545 and Roneparstat, are in active clinical development, the former in solid tumors, and the latter in Multiple Myeloma (MM). These progresses together with increasing and sound preclinical data suggesting a significant potential for anti-heparanase therapy in many types of tumors, underscores the need to explore the full potential of this novel and safe therapeutic approach. This paper reviews the role of heparanase as novel therapeutic target in cancer and illustrates Roneparstat as a concrete example of such potential.

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March 2017
19 Reads

Structural features of heparanase-inhibiting non-anticoagulant heparin derivative Roneparstat.

Carbohydr Polym 2017 Jan 13;156:470-480. Epub 2016 Sep 13.

Centro Alta Tecnologia Istituto di Ricerche Chimiche e Biochimiche G. Ronzoni, srl, via G. Colombo, 81, 20133 Milan, Italy; Istituto di Ricerche Chimiche e Biochimiche G.Ronzoni, via G. Colombo, 81, 20133 Milan, Italy.

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http://dx.doi.org/10.1016/j.carbpol.2016.09.032DOI Listing
January 2017
13 Reads
4.074 Impact Factor

Synthesis of ST7612AA1, a Novel Oral HDAC Inhibitor, via Radical 
Thioacetic Acid Addition.

Curr Bioact Compd 2016 Dec;12(4):282-288

R&D Sigma-Tau IFR S.p.A., Via Pontina Km 30,400, I-00071 Pomezia, Rome, Italy.

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http://dx.doi.org/10.2174/1573407212666160504160556DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5101637PMC
December 2016
29 Reads

Kinetic analysis and molecular modeling of the inhibition mechanism of roneparstat (SST0001) on human heparanase.

Glycobiology 2016 06 13;26(6):640-54. Epub 2016 Jan 13.

R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, Pomezia, Roma 00071, Italy.

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http://dx.doi.org/10.1093/glycob/cww003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4847616PMC
June 2016
16 Reads
3.147 Impact Factor

Heparanase: a rainbow pharmacological target associated to multiple pathologies including rare diseases.

Future Med Chem 2016 04 8;8(6):647-80. Epub 2016 Apr 8.

Medicinal Chemistry, R&D Sigma-Tau IFR S.p.A., via Pontina, km 30,400. I-00071 Pomezia (RM), Italy.

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http://dx.doi.org/10.4155/fmc-2016-0012DOI Listing
April 2016
58 Reads
4.000 Impact Factor

Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.

Eur J Med Chem 2016 Apr 3;112:99-105. Epub 2016 Feb 3.

Department of Food, Environmental and Nutritional Sciences, Division of Chemistry and Molecular Biology, University of Milan, via Celoria 2, 20133 Milan, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2016.02.001DOI Listing
April 2016
14 Reads
3.447 Impact Factor

Heparanase: a rainbow pharmacological target associated to multiple pathologies including rare diseases

Future Med. Chem. (2016) 8(6), 647–680

Future Med. Chem

In recent years, heparanase has attracted considerable attention as a promising target for innovative pharmacological applications. Heparanase is a multifaceted protein endowed with enzymatic activity, as an endo-β-d-glucuronidase, and nonenzymatic functions. It is responsible for the cleavage of heparan sulfate side chains of proteoglycans, resulting in structural alterations of the extracellular matrix. Heparanase appears to be involved in major human diseases, from the most studied tumors to chronic inflammation, diabetic nephropathy, bone osteolysis, thrombosis and atherosclerosis, in addition to more recent investigation in various rare diseases. The present review provides an overview on heparanase, its biological role, inhibitors and possible clinical applications, covering the latest findings in these areas.

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April 2016
14 Reads

The thioacetate-ω(γ-lactam carboxamide) HDAC inhibitor ST7612AA1 as HIV-1 latency reactivation agent.

Antiviral Res 2015 Nov 5;123:62-9. Epub 2015 Sep 5.

AIDS Research Institute - IrsiCaixa and Health Research Institute Germans Trias i Pujol (IGTP), Hospital Germans Trias i Pujol, Universitat Autònoma de Barcelona, Badalona, Spain. Electronic address:

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http://dx.doi.org/10.1016/j.antiviral.2015.09.004DOI Listing
November 2015
8 Reads
3.938 Impact Factor

The novel atypical retinoid ST5589 down-regulates Aurora Kinase A and has anti-tumour activity in lymphoma pre-clinical models.

Br J Haematol 2015 Nov 3;171(3):378-86. Epub 2015 Aug 3.

Lymphoma and Genomics Research Program, IOR Institute of Oncology Research, Bellinzona, Switzerland.

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http://dx.doi.org/10.1111/bjh.13595DOI Listing
November 2015
15 Reads
4.711 Impact Factor

Synthesis of 5,6-dihydro-4H-benzo[d]isoxazol-7-one and 5,6-dihydro-4H-isoxazolo[5,4-c]pyridin-7-one derivatives as potential Hsp90 inhibitors.

Chem Biol Drug Des 2015 Nov 30;86(5):1030-5. Epub 2015 Apr 30.

Department of Food, Environmental and Nutritional Sciences, Division of Chemistry and Molecular Biology, University of Milano, via Celoria 2, Milan, I-20133, Italy.

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http://dx.doi.org/10.1111/cbdd.12570DOI Listing
November 2015
10 Reads
2.485 Impact Factor

Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.

Bioorg Med Chem Lett 2015 Oct 5;25(20):4457-60. Epub 2015 Sep 5.

Department of Food, Environmental and Nutritional Sciences, University of Milan, Via Celoria 2, 20133 Milan, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2015.09.006DOI Listing
October 2015
15 Reads
2.420 Impact Factor

Ruthenium-catalyzed synthesis of 5-amino-1,2,3-triazole-4-carboxylates for triazole-based scaffolds: beyond the dimroth rearrangement.

J Org Chem 2015 Mar 16;80(5):2562-72. Epub 2015 Feb 16.

Dipartimento di Biotecnologie, Chimica e Farmacia, Università di Siena , Via A. Moro 2, 53100 Siena, Italy.

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http://dx.doi.org/10.1021/jo502577eDOI Listing
March 2015
15 Reads
4.721 Impact Factor

Targeting the invasive phenotype of cisplatin-resistant non-small cell lung cancer cells by a novel histone deacetylase inhibitor.

Biochem Pharmacol 2015 Mar 16;94(2):79-90. Epub 2015 Jan 16.

Molecular Pharmacology Unit, Fondazione IRCCS Istituto Nazionale per lo Studio e la Cura dei Tumori, Milan, Via Venezian 1/Via Amadeo 42, 20133 Milan, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.bcp.2015.01.002DOI Listing
March 2015
15 Reads
5.009 Impact Factor

Exploring in vitro and in vivo Hsp90 inhibitors activity against human protozoan parasites.

Bioorg Med Chem Lett 2015 Feb 20;25(3):462-5. Epub 2014 Dec 20.

R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, I-00040, Pomezia, Roma, Italy.

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http://dx.doi.org/10.1016/j.bmcl.2014.12.048DOI Listing
February 2015
7 Reads
2.420 Impact Factor

Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.

Bioorg Med Chem Lett 2015 Feb 19;25(3):459-61. Epub 2014 Dec 19.

R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, I-00040 Pomezia, Roma, Italy.

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http://dx.doi.org/10.1016/j.bmcl.2014.12.051DOI Listing
February 2015
8 Reads
2.420 Impact Factor

ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.

J Med Chem 2014 Oct 8;57(20):8358-77. Epub 2014 Oct 8.

R&D Sigma-Tau Industrie Farmaceutiche Riunite SpA , Via Pontina Km 30,400, I-00040 Pomezia, Roma, Italy.

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http://dx.doi.org/10.1021/jm5008209DOI Listing
October 2014
18 Reads
5.447 Impact Factor

Preclinical antitumor activity of SST0116CL1: a novel heat shock protein 90 inhibitor.

Int J Oncol 2014 Oct 1;45(4):1421-9. Epub 2014 Aug 1.

Research & Development, Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Pomezia, Italy.

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http://dx.doi.org/10.3892/ijo.2014.2575DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4151799PMC
October 2014
11 Reads
3.025 Impact Factor

ST7612AA1, a Thioacetate-ω(γ-lactam carboxamide) Derivative

J Med Chem. 2014, 57(20):8358-8377

Journal of Medicinal Chemistry

A systematic study of medicinal chemistry aimed at identifying a new generation of HDAC inhibitors, through the introduction of a thiol zinc-binding group (ZBG) and of an amide-lactam in the ω-position of the polyethylene chain of the vorinostat scaffold, allowed the selection of a new class of potent pan-HDAC inhibitors (pan-HDACis). Simple, highly versatile, and efficient synthetic approaches were used to synthesize a library of these new derivatives, which were then submitted to a screening for HDAC inhibition as well as to a preliminary in vitro assessment of their antiproliferative activity. Molecular docking into HDAC crystal structures suggested a binding mode for these thiol derivatives consistent with the stereoselectivity observed upon insertion of amide-lactam substituents in the ω-position. ST7612AA1 (117), selected as a drug candidate for further development, showed an in vitro activity in the nanomolar range associated with a remarkable in vivo antitumor activity, highly competitive with the most potent HDAC inhibitors, currently under clinical trials. A preliminary study of PK and metabolism is also illustrated.

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October 2014
13 Reads

Preclinical antitumor activity of SST0116CL1: A novel heat shock protein 90 inhibitor

Inter. J. Oncology, 2014, 45(4), 1421-1429

International Journal of Oncology

4-Amino substituted resorcino-isoxazole (SST0116CL1) (property of Sigma-Tau Research Switzerland S.A.) is a potent, second generation, small-molecule heat shock protein 90 inhibitor (Hsp90i). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein degradation and tumor growth inhibition. The aim of the study was to assess SST0116CL1 in various solid and haematological tumors. The antitumor properties of SST0116CL1 were assessed using in vitro cell proliferation and client protein degradation assays and in vivo different tumor xenograft models. Pharmacokinetic (PK) data were also generated in tumor-bearing mice to gain an understanding of optimal dosing schedules and regimens. SST0116CL1 was shown to inhibit recombinant Hsp90α and to induce the destabilization of different client proteins, often overexpressed and constitutively activated in different types of hematological or solid human tumors. In preclinical in vivo studies, it was revealed to induce antitumor effects in murine models of leukemia and of gastric and ovarian carcinoma. A modulation of PD biomarkers in terms of downregulation of Hsp90 client proteins in tumor-bearing mice was found. SST0116CL1 is a new clinical candidate for cancer therapy. The antitumor property of SST0116CL1, likely due to direct inhibition of the Hsp90 enzymatic activity, may prove to be a critical attribute as the compound enters phase I clinical trials.

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August 2014
11 Reads

Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.

Eur J Med Chem 2014 May 8;79:251-9. Epub 2014 Apr 8.

Department of Food, Environmental and Nutritional Sciences, Division of Chemistry and Molecular Biology, Università di Milano, Via Celoria 2, 20133 Milano, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.04.021DOI Listing
May 2014
12 Reads
3.447 Impact Factor

Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.

J Med Chem 2014 Mar 17;57(6):2258-74. Epub 2014 Mar 17.

Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena , Via A. Moro 2, I-53100 Siena, Italy.

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http://dx.doi.org/10.1021/jm401536bDOI Listing
March 2014
18 Reads
5.447 Impact Factor

7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors.

Bioorg Med Chem 2014 Feb 22;22(3):1089-103. Epub 2013 Dec 22.

Department of Food, Environmental and Nutritional Sciences, Division of Chemistry and Molecular Biology, Università di Milano, via Celoria 2, 20133 Milano, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2013.12.031DOI Listing
February 2014
6 Reads
2.793 Impact Factor

Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold.

Bioorg Med Chem Lett 2014 Jan 18;24(2):462-6. Epub 2013 Dec 18.

Department of Food, Environmental and Nutritional Sciences, Division of Chemistry and Molecular Biology, Università di Milano, Via Celoria 2, 20133 Milano, Italy.

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http://dx.doi.org/10.1016/j.bmcl.2013.12.048DOI Listing
January 2014
12 Reads
2.420 Impact Factor

Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors.

Bioorg Med Chem Lett 2014 Jan 4;24(1):61-4. Epub 2013 Dec 4.

R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, I-00040 Pomezia, Roma, Italy.

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http://dx.doi.org/10.1016/j.bmcl.2013.11.072DOI Listing
January 2014
9 Reads
2.420 Impact Factor

Camptothecins in tumor homing via an RGD sequence mimetic.

Bioorg Med Chem Lett 2012 Oct 26;22(20):6509-12. Epub 2012 Jul 26.

Corporate R&D, sigma-tau Industrie Farmaceutiche Riunite SpA, Pomezia, Italy.

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http://dx.doi.org/10.1016/j.bmcl.2012.07.061DOI Listing
October 2012
5 Reads
2.420 Impact Factor

Histone deacetylase inhibitors in the treatment of cancer: overview and perspectives.

Future Med Chem 2012 Jul;4(11):1439-60

Medicinal Chemistry, Oncology, R&D, Corporate Sigma-Tau S.p.A, Via Pontina km 30, Pomezia, Italy.

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http://www.reactionbiology.com/webapps/site/NewsPDFs/Histone
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http://www.future-science.com/doi/10.4155/fmc.12.80
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http://dx.doi.org/10.4155/fmc.12.80DOI Listing
July 2012
18 Reads
4.000 Impact Factor

New retinoid derivatives as back-ups of Adarotene.

Bioorg Med Chem 2012 Apr 6;20(7):2405-15. Epub 2012 Feb 6.

Sigma-Tau Industrie Farmaceutiche Riunite Spa, via Pontina Km 30.400, 00040 Pomezia, Italy.

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http://dx.doi.org/10.1016/j.bmc.2012.01.042DOI Listing
April 2012
7 Reads
2.793 Impact Factor

Oxime amides as a novel zinc binding group in histone deacetylase inhibitors: synthesis, biological activity, and computational evaluation.

J Med Chem 2011 Apr 18;54(7):2165-82. Epub 2011 Mar 18.

Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via A. Moro 2, I-53100 Siena, Italy.

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http://dx.doi.org/10.1021/jm101373aDOI Listing
April 2011
12 Reads
5.447 Impact Factor

Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.

J Med Chem 2010 Dec 12;53(23):8387-99. Epub 2010 Nov 12.

Department of Chemistry, Université de Montréal, P.O. Box 6128, Station Centre-ville, Montréal, QC, H3C 3J7 Canada.

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http://dx.doi.org/10.1021/jm101092uDOI Listing
December 2010
8 Reads
5.447 Impact Factor

Natural and semisynthetic azaphilones as a new scaffold for Hsp90 inhibitors.

Bioorg Med Chem 2010 Aug 1;18(16):6031-43. Epub 2010 Jul 1.

Dipartimento di Scienze Molecolari Agroalimentari, Università di Milano, Via Celoria 2, 20133 Milano, Italy.

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http://dx.doi.org/10.1016/j.bmc.2010.06.068DOI Listing
August 2010
17 Reads
2.793 Impact Factor

Vorinostat-like molecules as structural, stereochemical, and pharmacological tools.

ACS Med Chem Lett 2010 May 11;1(2):70-4. Epub 2010 Mar 11.

Sigma-Tau Research & Development, Via Pontina Km 30.400, I-00040 Pomezia, Roma, Italy.

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http://dx.doi.org/10.1021/ml100028gDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4007911PMC
May 2010
9 Reads
3.120 Impact Factor

Novel tumor-targeted RGD peptide-camptothecin conjugates: synthesis and biological evaluation.

Bioorg Med Chem 2010 Jan 12;18(1):64-72. Epub 2009 Nov 12.

Istituto di Ricerche Chimiche e Biochimiche G.Ronzoni, via G Colombo 81, 20133 Milano, Italy.

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http://dx.doi.org/10.1016/j.bmc.2009.11.019DOI Listing
January 2010
20 Reads
2.793 Impact Factor

Azetidinones as zinc-binding groups to design selective HDAC8 inhibitors.

ChemMedChem 2009 Dec;4(12):1991-2001

Dipartimento di Chimica G. Ciamician, Università of Bologna, Via Selmi 2, 40126 Bologna, Italy.

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http://dx.doi.org/10.1002/cmdc.200900309DOI Listing
December 2009
10 Reads
2.968 Impact Factor

Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors.

Bioorg Med Chem Lett 2009 May 26;19(10):2840-3. Epub 2009 Mar 26.

Sigma-Tau Research and Development, Pomezia, Roma, Italy.

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http://dx.doi.org/10.1016/j.bmcl.2009.03.101DOI Listing
May 2009
11 Reads
2.420 Impact Factor

E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation.

Bioorg Med Chem Lett 2008 May 30;18(9):2910-5. Epub 2008 Mar 30.

Sigma-Tau Research & Development, Via Pontina Km 30.400, I-00040 Pomezia, Rome, Italy.

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http://dx.doi.org/10.1016/j.bmcl.2008.03.074DOI Listing
May 2008
16 Reads
2.420 Impact Factor

Synthesis and biological activity of fluorinated combretastatin analogues.

J Med Chem 2008 May 9;51(9):2708-21. Epub 2008 Apr 9.

R&D, Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30.400, 00040 Pomezia, Italy.

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http://dx.doi.org/10.1021/jm701362mDOI Listing
May 2008
12 Reads
5.447 Impact Factor

Synthesis and DNA-cleaving activity of lactenediynes conjugated with DNA-complexing moieties.

Bioorg Med Chem 2008 Apr 13;16(7):3501-18. Epub 2008 Feb 13.

Dipartimento di Chimica e Chimica Industriale, via Dodecaneso 31, I-16146 Genova, Italy.

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http://dx.doi.org/10.1016/j.bmc.2008.02.022DOI Listing
April 2008
5 Reads
2.793 Impact Factor

Microbial transformation of spirolaxine, a bioactive undecaketide fungal metabolite from the basidiomycete Sporotrichum laxum.

Chem Biodivers 2007 Dec;4(12):2772-9

CNR-ICRM, Department of Chemistry, Materials and Chemical Engineering, Politecnico di Milano, via Mancinelli, 7, I-20123, Milano.

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http://dx.doi.org/10.1002/cbdv.200790226DOI Listing
December 2007
8 Reads
1.515 Impact Factor

Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence.

Bioorg Med Chem Lett 2007 Nov 8;17(22):6261-5. Epub 2007 Sep 8.

Department of Chemistry, Université de Montréal, Station Centre-ville, Montréal, Quebec, Canada.

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http://dx.doi.org/10.1016/j.bmcl.2007.09.014DOI Listing
November 2007
5 Reads
2.420 Impact Factor

Synthesis and structure-activity relationships of new antiproliferative and proapoptotic retinoid-related biphenyl-4-yl-acrylic acids.

Bioorg Med Chem 2007 Jul 3;15(14):4863-75. Epub 2007 May 3.

Dipartimento di Scienze Molecolari Agroalimentari, Università di Milano, Via Celoria 2, 20133 Milano, Italy.

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http://dx.doi.org/10.1016/j.bmc.2007.04.057DOI Listing
July 2007
8 Reads
2.793 Impact Factor

Exploring alternative Zn-binding groups in the design of HDAC inhibitors: squaric acid, N-hydroxyurea, and oxazoline analogues of SAHA.

Bioorg Med Chem Lett 2006 Sep 25;16(18):4784-7. Epub 2006 Jul 25.

Department of Chemistry, Université de Montréal, PO Box 6128, Station Centre-ville, Montréal, Que., Canada H3C 3J7.

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http://dx.doi.org/10.1016/j.bmcl.2006.06.090DOI Listing
September 2006
6 Reads
2.420 Impact Factor

Synthesis and cytotoxic activity of polyamine analogues of camptothecin.

J Med Chem 2006 Aug;49(17):5177-86

Dipartimento di Scienze Molecolari Agroalimentari, Università di Milano, Via Celoria 2, 20133 Milano, Italy.

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http://dx.doi.org/10.1021/jm060285bDOI Listing
August 2006
9 Reads
5.447 Impact Factor

Novel combretastatin analogues endowed with antitumor activity.

J Med Chem 2006 Jun;49(11):3143-52

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17/19, 44100 Ferrara, Italy.

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http://dx.doi.org/10.1021/jm0510732DOI Listing
June 2006
14 Reads
5.447 Impact Factor

Targeting integrins: insights into structure and activity of cyclic RGD pentapeptide mimics containing azabicycloalkane amino acids.

Bioorg Med Chem 2006 Jan 7;14(1):169-80. Epub 2005 Oct 7.

Dipartimento di Chimica Organica e Industriale and Centro Interdisciplinare Studi bio-molecolari e applicazioni Industriali, (CISI), Università degli Studi di Milano, via G. Venezian 21, I-20133 Milan, Italy.

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http://dx.doi.org/10.1016/j.bmc.2005.08.048DOI Listing
January 2006
14 Reads
2.793 Impact Factor

Biological and molecular properties of a new alpha(v)beta3/alpha(v)beta5 integrin antagonist.

Mol Cancer Ther 2005 Nov;4(11):1670-80

Organic and Industrial Chemistry Department, Centre for Biomolecular Interdisciplinary Studies and Industrial Applications, University of Milan, Italy.

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http://dx.doi.org/10.1158/1535-7163.MCT-05-0120DOI Listing
November 2005
14 Reads
5.683 Impact Factor

Modulation of the heparanase-inhibiting activity of heparin through selective desulfation, graded N-acetylation, and glycol splitting.

J Biol Chem 2005 Apr 12;280(13):12103-13. Epub 2005 Jan 12.

G. Ronzoni Institute for Chemical and Biochemical Research, via G. Colombo, 81, 20133 Milan, Italy.

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http://dx.doi.org/10.1074/jbc.M414217200DOI Listing
April 2005
25 Reads
4.573 Impact Factor

A novel atypical retinoid endowed with proapoptotic and antitumor activity.

J Med Chem 2003 Mar;46(6):909-12

Dipartimento di Scienze Molecolari Agroalimentari, Università di Milano, Milano, Italy.

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http://dx.doi.org/10.1021/jm025593yDOI Listing
March 2003
7 Reads
5.447 Impact Factor

Fluorinated anthracyclines: synthesis and biological activity.

Curr Med Chem 2002 Mar;9(6):687-712

Dept. of Chemistry - Sigma-Tau, via Pontina Km 30, (Rome), 400 I-00040 Pomezia, Italy.

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March 2002
6 Reads
3.853 Impact Factor

Growth inhibition of human ovarian carcinoma by a novel AvidinOX-anchored biotinylated camptothecin derivative.

Bioorg Med Chem Lett. 2018 Sep 15

Bioorganic Med Chem Lett

Oxidized form of avidin, named AvidinOX, provides stable fixation of biotinylated molecules in tissues thus representing a breakthrough in topical treatment of cancer. AvidinOX proved to be a stable receptor for radiolabeled biotin, biotinylated antibodies and cells. In order to expand applicability of the AvidinOX-based delivery platform, in the present study we investigated the possibility to hold biotinylated chemotherapeutics in AvidinOX-treated sites. A novel biotinylated gimatecan-derived camptothecin, coded ST8161AA1, was injected at suboptimal doses into human tumors xenografted in mice alone or pre-complexed to AvidinOX. Significantly higher growth inhibition was observed when the drug was anchored to AvidinOX suggesting the potential utility of this delivery modality for the local treatment of inoperable tumors.

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Top co-authors

Claudio Pisano
Claudio Pisano

Research Institute

30
Loredana Vesci
Loredana Vesci

R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

28
Walter Cabri
Walter Cabri

Analytical Development

18
Sabrina Dallavalle
Sabrina Dallavalle

Università di Milano

16
Gianfranco Battistuzzi
Gianfranco Battistuzzi

R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

15
Sergio Penco
Sergio Penco

Ronzoni Institute for Chemical and Biochem. Research

13
Franco Zunino
Franco Zunino

Molecular Pharmacology Unit

12
Raffaella Cincinelli
Raffaella Cincinelli

Università di Milano

11
Loana Musso
Loana Musso

University of Milan

11