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. 2008 Dec 15;18(24):6482-5.
doi: 10.1016/j.bmcl.2008.10.058. Epub 2008 Oct 17.

Alpha-mercaptoketone based histone deacetylase inhibitors

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

Alpha-mercaptoketone based histone deacetylase inhibitors

Paul L Wash et al. Bioorg Med Chem Lett. .

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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