α-Mercaptoketone based histone deacetylase inhibitors

Bioorganic & Medicinal Chemistry Letters
2008.0

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.

DOI： 10.1016/j.bmcl.2008.10.058

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