Literature DB >> 19441846

Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.

Olaf Kinzel1, Laura Llauger-Bufi, Giovanna Pescatore, Michael Rowley, Carsten Schultz-Fademrecht, Edith Monteagudo, Massimiliano Fonsi, Odalys Gonzalez Paz, Fabrizio Fiore, Christian Steinkühler, Philip Jones.   

Abstract

The optimization of a potent, class I selective ketone HDAC inhibitor is shown. It possesses optimized pharmacokinetic properties in preclinical species, has a clean off-target profile, and is negative in a microbial mutagenicity (Ames) test. In a mouse xenograft model it shows efficacy comparable to that of vorinostat at a 10-fold reduced dose.

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Year:  2009        PMID： 19441846     DOI： 10.1021/jm9004303

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  11 in total

1.  The DNA damage mark pH2AX differentiates the cytotoxic effects of small molecule HDAC inhibitors in ovarian cancer cells.

Authors:  Andrew J Wilson; Edward Holson; Florence Wagner; Yan-Ling Zhang; Daniel M Fass; Stephen J Haggarty; Srividya Bhaskara; Scott W Hiebert; Stuart L Schreiber; Dineo Khabele
Journal:  Cancer Biol Ther       Date:  2011-09-15       Impact factor: 4.742

2.  Class I HDAC Inhibitors Display Different Antitumor Mechanism in Leukemia and Prostatic Cancer Cells Depending on Their p53 Status.

Authors:  Xiaoyang Li; Yuri K Peterson; Elizabeth S Inks; Richard A Himes; Jiaying Li; Yingjie Zhang; Xiujie Kong; C James Chou
Journal:  J Med Chem       Date:  2018-03-09       Impact factor: 7.446

3.  Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.

Authors:  Alberto Bresciani; Jesus M Ontoria; Ilaria Biancofiore; Antonella Cellucci; Alina Ciammaichella; Annalise Di Marco; Federica Ferrigno; Alessandra Francone; Savina Malancona; Edith Monteagudo; Emanuela Nizi; Paola Pace; Simona Ponzi; Ilaria Rossetti; Maria Veneziano; Vincenzo Summa; Steven Harper
Journal:  ACS Med Chem Lett       Date:  2018-11-27       Impact factor: 4.345

4.  Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.

Authors:  Jesus M Ontoria; Giacomo Paonessa; Simona Ponzi; Federica Ferrigno; Emanuela Nizi; Ilaria Biancofiore; Savina Malancona; Rita Graziani; David Roberts; Paul Willis; Alberto Bresciani; Nadia Gennari; Ottavia Cecchetti; Edith Monteagudo; Maria V Orsale; Maria Veneziano; Annalise Di Marco; Antonella Cellucci; Ralph Laufer; Sergio Altamura; Vincenzo Summa; Steven Harper
Journal:  ACS Med Chem Lett       Date:  2016-03-05       Impact factor: 4.345

5.  Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.

Authors:  Rong He; Yufeng Chen; Yihua Chen; Andrei V Ougolkov; Jin-San Zhang; Doris N Savoy; Daniel D Billadeau; Alan P Kozikowski
Journal:  J Med Chem       Date:  2010-02-11       Impact factor: 7.446

6.  Chemical probes of a trisubstituted pyrrole to identify its protein target(s) in Plasmodium sporozoites.

Authors:  Tyrell Towle; Isabell Chang; Isabel Chang; Robert J Kerns; Purnima Bhanot
Journal:  Bioorg Med Chem Lett       Date:  2013-01-11       Impact factor: 2.823

7.  Synthesis of HDAC Inhibitor Libraries via Microscale Workflow.

Authors:  Kevin D Dykstra; Eric Streckfuss; Min Liu; Jian Liu; Younong Yu; Ming Wang; Joseph A Kozlowski; Robert W Myers; Alexei V Buevich; Milana M Maletic; Petr Vachal; Shane W Krska
Journal:  ACS Med Chem Lett       Date:  2021-02-08       Impact factor: 4.345

8.  Exploration of Novel Inhibitors for Class I Histone Deacetylase Isoforms by QSAR Modeling and Molecular Dynamics Simulation Assays.

Authors:  Zainab Noor; Noreen Afzal; Sajid Rashid
Journal:  PLoS One       Date:  2015-10-02       Impact factor: 3.240

9.  Hydroxyl Ketone-Based Histone Deacetylase Inhibitors To Gain Insight into Class I HDAC Selectivity versus That of HDAC6.

Authors:  Mohamed D M Traoré; Vincent Zwick; Claudia A Simões-Pires; Alessandra Nurisso; Mark Issa; Muriel Cuendet; Marjorie Maynadier; Sharon Wein; Henri Vial; Helene Jamet; Yung-Sing Wong
Journal:  ACS Omega       Date:  2017-04-20

10.  Butyrate histone deacetylase inhibitors.

Authors:  Kosta Steliou; Michael S Boosalis; Susan P Perrine; José Sangerman; Douglas V Faller
Journal:  Biores Open Access       Date:  2012-08
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