2. Academic Validation
  3. Optimization of a series of potent and selective ketone histone deacetylase inhibitors

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

Affiliation

  • 1 IRBM/Merck Research Laboratories, Via Pontina km 30,600, 00040 Pomezia, Italy. giovanna_pescatore@merck.com
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.

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