Marina Ciomei

Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515.

Authors:

Gianluca Papeo Paolo Orsini Nilla R Avanzi Daniela Borghi Elena Casale Marina Ciomei Alessandra Cirla Viviana Desperati Daniele Donati Eduard R Felder Arturo Galvani Marco Guanci Antonella Isacchi Helena Posteri Sonia Rainoldi Federico Riccardi-Sirtori Alessandra Scolaro Alessia Montagnoli

ACS Med Chem Lett 2019 Apr 13;10(4):534-538. Epub 2019 Mar 13.

Oncology, Nerviano Medical Sciences S.r.l., Viale Pasteur 10, 20014 Nerviano, Milan, Italy.

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April 2019

Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications.

Mol Cancer Ther 2016 04 3;15(4):628-39. Epub 2016 Mar 3.

Nerviano Medical Sciences srl, Nerviano, Milan, Italy.

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April 2016

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.

J Med Chem 2015 Sep 26;58(17):6875-98. Epub 2015 Aug 26.

Oncology, Nerviano Medical Sciences Srl , Viale Pasteur 10, 20014 Nerviano, Milan, Italy.

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September 2015

Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders.

Authors:

Maria Gabriella Brasca Paola Gnocchi Marcella Nesi Nadia Amboldi Nilla Avanzi Jay Bertrand Simona Bindi Giulia Canevari Daniele Casero Marina Ciomei Nicoletta Colombo Sabrina Cribioli Gabriele Fachin Eduard R Felder Arturo Galvani Antonella Isacchi Ilaria Motto Achille Panzeri Daniele Donati

Bioorg Med Chem 2015 May 28;23(10):2387-407. Epub 2015 Mar 28.

Nerviano Medical Sciences S.r.l., Oncology, Viale Pasteur 10, 20014 Nerviano (MI), Italy.

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May 2015

Optimization of diarylthiazole B-raf inhibitors: identification of a compound endowed with high oral antitumor activity, mitigated hERG inhibition, and low paradoxical effect.

Authors:

Maurizio Pulici Gabriella Traquandi Chiara Marchionni Michele Modugno Rosita Lupi Nadia Amboldi Elena Casale Nicoletta Colombo Luca Corti Marina Fasolini Fabio Gasparri Wilma Pastori Alessandra Scolaro Daniele Donati Eduard Felder Arturo Galvani Antonella Isacchi Enrico Pesenti Marina Ciomei

ChemMedChem 2015 Feb 27;10(2):276-95. Epub 2014 Nov 27.

Nerviano Medical Sciences Srl, Business Unit Oncology, Viale Pasteur 10, 20014 Nerviano (MI) (Italy).

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February 2015

Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.

Bioorg Med Chem 2014 Sep 21;22(17):4998-5012. Epub 2014 Jun 21.

Nerviano Medical Sciences S.r.l., Oncology, Viale Pasteur 10, 20014 Nerviano (MI), Italy.

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September 2014

NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases.

Clin Cancer Res 2013 Jul 14;19(13):3520-32. Epub 2013 May 14.

Department of Biotechnology, Nerviano Medical Sciences Srl, Nerviano (MI), Italy.

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July 2013

Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhibitor PHA-848125.

Authors:

Simona Caporali Ester Alvino Lauretta Levati Alessia I Esposito Marina Ciomei Maria G Brasca Donatella Del Bufalo Marianna Desideri Enzo Bonmassar Ulrich Pfeffer Stefania D'Atri

Biochem Pharmacol 2012 Sep 13;84(5):598-611. Epub 2012 Jun 13.

Laboratory of Molecular Oncology, Istituto Dermopatico dell'Immacolata-IRCCS, Via dei Monti di Creta 104, 00167 Rome, Italy.

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September 2012

Phase I study of the safety, tolerability and pharmacokinetics of PHA-848125AC, a dual tropomyosin receptor kinase A and cyclin-dependent kinase inhibitor, in patients with advanced solid malignancies.

Authors:

Glen J Weiss Manuel Hidalgo Mitesh J Borad Daniel Laheru Raoul Tibes Ramesh K Ramanathan Lisa Blaydorn Gayle Jameson Antonio Jimeno Jeffrey D Isaacs Angela Scaburri Maria Adele Pacciarini Francesco Fiorentini Marina Ciomei Daniel D Von Hoff

Invest New Drugs 2012 Dec 9;30(6):2334-43. Epub 2011 Dec 9.

Virginia G. Piper Cancer Center at Scottsdale Healthcare (VGPCC), Scottsdale, AZ 85258, USA.

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December 2012

Miniaturizing bromodeoxyuridine incorporation enables the usage of flow cytometry for cell cycle analysis of adherent tissue culture cells for high throughput screening.

Authors:

Paolo Cappella Maria Laura Giorgini Claudia Ernestina Re Paolo Ubezio Marina Ciomei Jürgen Moll

Cytometry A 2010 Oct 8;77(10):953-61. Epub 2010 Sep 8.

Cell Biology Department, Nerviano Medical Sciences Srl, Nerviano, Italy.

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October 2010

Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy.

Authors:

Clara Albanese Rachele Alzani Nadia Amboldi Nilla Avanzi Dario Ballinari Maria Gabriella Brasca Claudio Festuccia Francesco Fiorentini Giuseppe Locatelli Wilma Pastori Veronica Patton Fulvia Roletto Francesco Colotta Arturo Galvani Antonella Isacchi Jurgen Moll Enrico Pesenti Ciro Mercurio Marina Ciomei

Mol Cancer Ther 2010 Aug 3;9(8):2243-54. Epub 2010 Aug 3.

Cell Biology Department, BU Oncology, Nerviano Medical Sciences, v.le Pasteur 10, Nerviano, Milan 20014, Italy.

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August 2010

Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study.

Authors:

Giuseppe Locatelli Roberta Bosotti Marina Ciomei Maria G Brasca Raffaele Calogero Ciro Mercurio Francesco Fiorentini Matteo Bertolotti Emanuela Scacheri Angela Scaburri Arturo Galvani Enrico Pesenti Thierry De Baere Jean-Charles Soria Vladimir Lazar Antonella Isacchi

Mol Cancer Ther 2010 May 27;9(5):1265-73. Epub 2010 Apr 27.

Business Unit Oncology, Nerviano Medical Sciences srl, Nerviano (MI), Italy.

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May 2010

Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-Ras(G12D)LA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging.

Authors:

Anna Degrassi Micaela Russo Cristina Nanni Veronica Patton Rachele Alzani Anna M Giusti Stefano Fanti Marina Ciomei Enrico Pesenti Gemma Texido

Mol Cancer Ther 2010 Mar 2;9(3):673-81. Epub 2010 Mar 2.

Pharmacology Department, BU Oncology, Nerviano Medical Sciences, Milano, Italy.

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March 2010

Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia models.

Authors:

Rachele Alzani Olga Pedrini Clara Albanese Roberta Ceruti Alessia Casolaro Veronica Patton Francesco Colotta Alessandro Rambaldi Martino Introna Enrico Pesenti Marina Ciomei Josée Golay

Exp Hematol 2010 Apr 16;38(4):259-269.e2. Epub 2010 Feb 16.

Nerviano Medical Sciences Srl, Business Unit Oncology, Nerviano, Italy.

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April 2010

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

Bioorg Med Chem 2010 Mar 25;18(5):1844-53. Epub 2010 Jan 25.

Nerviano Medical Sciences Srl, Business Unit Oncology, Viale Pasteur 10, 20014 Nerviano (MI), Italy.

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March 2010

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.

Authors:

Gabriella Traquandi Marina Ciomei Dario Ballinari Elena Casale Nicoletta Colombo Valter Croci Francesco Fiorentini Antonella Isacchi Antonio Longo Ciro Mercurio Achille Panzeri Wilma Pastori Paolo Pevarello Daniele Volpi Patrick Roussel Anna Vulpetti Maria Gabriella Brasca

J Med Chem 2010 Mar;53(5):2171-87

Nerviano Medical Sciences Srl, Business Unit Oncology, Viale Pasteur 10, 20014 Nerviano, MI, Italy.

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March 2010

The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound.

Authors:

Simona Caporali Ester Alvino Giuseppe Starace Marina Ciomei Maria Gabriella Brasca Lauretta Levati Alberto Garbin Daniele Castiglia Claudia Covaciu Enzo Bonmassar Stefania D'Atri

Pharmacol Res 2010 May 21;61(5):437-48. Epub 2009 Dec 21.

Laboratory of Molecular Oncology, Istituto Dermopatico dell'Immacolata-IRCCS, Via dei Monti di Creta 104, 00167 Rome, Italy.

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May 2010

Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.

J Med Chem 2009 Aug;52(16):5152-63

Business Unit Oncology, Nerviano Medical Sciences Srl, Viale Pasteur 10, 20014 Nerviano (MI), Italy.

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August 2009

Antitumor activity of edotecarin in breast carcinoma models.

Authors:

Marina Ciomei Valter Croci Fabio Stellari Nadia Amboldi Rosa Giavarini Enrico Pesenti

Cancer Chemother Pharmacol 2007 Jul 7;60(2):229-35. Epub 2006 Nov 7.

Cell Biology/Oncology, Nerviano Medical Sciences, Viale Pasteur, 10, 20014 Nerviano (MI), Italy.

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July 2007

Antitumor efficacy of edotecarin as a single agent and in combination with chemotherapy agents in a xenograft model.

Authors:

Marina Ciomei Valter Croci Antonella Ciavolella Dario Ballinari Enrico Pesenti

Clin Cancer Res 2006 May;12(9):2856-61

Department of Biology, Drug Discovery Oncology, Nerviano Medical Sciences, Nerviano, Milan, Italy.

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May 2006

3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.

Authors:

Paolo Pevarello Daniele Fancelli Anna Vulpetti Raffaella Amici Manuela Villa Valeria Pittalà Paola Vianello Alexander Cameron Marina Ciomei Ciro Mercurio James R Bischoff Fulvia Roletto Mario Varasi Maria Gabriella Brasca

Bioorg Med Chem Lett 2006 Feb 14;16(4):1084-90. Epub 2005 Nov 14.

Department of Chemistry, Nerviano Medical Science, BU-Oncology, Via Pasteur 10, 20014 Nerviano MI, Italy.

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February 2006

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.

J Med Chem 2005 Apr;48(8):2944-56

Department Chemistry, Nerviano Medical Sciences, BU-Oncology and BU-Preclinical Science, Viale Pasteur 10, 20014 Nerviano (MI), Italy.

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April 2005

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.

J Med Chem 2004 Jun;47(13):3367-80

Chemistry Department, Pharmacia Italia, Viale Pasteur 10, 20014 Nerviano (MI), Italy.

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June 2004

Multiple effects of paclitaxel are modulated by a high c-myc amplification level.

Authors:

Maria Grazia Bottone Cristiana Soldani Gianluca Tognon Chiara Gorrini M Claudia Lazzè Olivier Brison Marina Ciomei Carlo Pellicciari A Ivana Scovassi

Exp Cell Res 2003 Oct;290(1):49-59

Dipartimento di Biologia Animale, Università di Pavia, Italy.

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October 2003

Endothelial cells overexpressing basic fibroblast growth factor (FGF-2) induce vascular tumors in immunodeficient mice.

Authors:

Francesco Sola Anna Gualandris Mirella Belleri Roberta Giuliani Daniela Coltrini Maria Bastaki Maria Pia Molinari Tosatti Fabrizio Bonardi Annunciata Vecchi Francesca Fioretti Marina Ciomei Maria Grandi Alberto Mantovani Marco Presta

Angiogenesis 1997 ;1(1):102-116

Pharmacia-Upjohn, Nerviano, 20014 Milan, Italy.

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January 1997

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