2. Academic Validation
  3. Alpha-mercaptoketone based histone deacetylase inhibitors

Alpha-mercaptoketone based histone deacetylase inhibitors

  • Bioorg Med Chem Lett. 2008 Dec 15;18(24):6482-5. doi: 10.1016/j.bmcl.2008.10.058.
Paul L Wash 1,  Timothy Z Hoffman,  Brandon M Wiley,  Céline Bonnefous,  Nicholas D Smith,  Michael S Sertic,  Charles M Lawrence,  Kent T Symons,  Phan-Manh Nguyen,  Kevin D Lustig,  Xin Guo,  Tami Annable,  Stewart A Noble,  Jeffrey H Hager,  Christian A Hassig,  James W Malecha
Affiliations

Affiliation

  • 1 Department of Chemistry, Kalypsys, Inc., 10420 Wateridge Circle, San Diego, CA 92121, USA.
PMID: 18954984 DOI: 10.1016/j.bmcl.2008.10.058
Abstract

In an effort to discover novel non-hydroxamic acid histone deacetylase (HDAC) inhibitors, a novel alpha-mercaptoketone was identified in a high-throughput screen. Lead optimization of the screening hit, led to a number of potent HDAC inhibitors. In particular, alpha-mercaptoketone 19y (KD5150) exhibited nanomolar in vitro activity and inhibition of tumor growth in vivo.

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