e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
α-Mercaptoketone based histone deacetylase inhibitors
PL Wash, TZ Hoffman, BM Wiley, C Bonnefous…
Index: Wash, Paul L.; Hoffman, Timothy Z.; Wiley, Brandon M.; Bonnefous, Celine; Smith, Nicholas D.; Sertic, Michael S.; Lawrence, Charles M.; Symons, Kent T.; Nguyen, Phan-Manh; Lustig, Kevin D.; Guo, Xin; Annable, Tami; Noble, Stewart A.; Hager, Jeffrey H.; Hassig, Christian A.; Malecha, James W. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 24 p. 6482 - 6485
In an effort to discover novel non-hydroxamic acid histone deacetylase (HDAC) inhibitors, a novel α-mercaptoketone was identified in a high-throughput screen. Lead optimization of the screening hit, led to a number of potent HDAC inhibitors. In particular, α-mercaptoketone 19y (KD5150) exhibited nanomolar in vitro activity and inhibition of tumor growth in vivo.
