Optimization of a series of potent and selective ketone histone deacetylase inhibitors

  • Bioorg Med Chem Lett. 2008 Oct 15;18(20):5528-32. doi: 10.1016/j.bmcl.2008.09.003.
Giovanna Pescatore  1 ,  Olaf Kinzel ,  Barbara Attenni ,  Ottavia Cecchetti ,  Fabrizio Fiore ,  Massimiliano Fonsi ,  Michael Rowley ,  Carsten Schultz-Fademrecht ,  Sergio Serafini ,  Christian Steinkühler ,  Philip Jones
Affiliations
  • 1. IRBM/Merck Research Laboratories, Via Pontina km 30,600, 00040 Pomezia, Italy. [email protected]
PMID: 18809328 DOI: 10.1016/j.bmcl.2008.09.003
Abstract

Histone deacetylase (HDAC) inhibitors offer a promising strategy for Cancer therapy and the first generation HDAC inhibitors are currently in the clinic. Herein we describe the optimization of a series of ketone small molecule HDAC inhibitors leading to potent and selective class I HDAC inhibitors with good dog PK.