Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors |
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Authors: | Anandan Sampath-Kumar Ward John S Brokx Richard D Bray Mark R Patel Dinesh V Xiao Xiao-Xi |
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Institution: | Miikana Therapeutics Inc, 6519 Dumbarton Circle, Fremont, CA 94555, USA. skumar@miikana.com |
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Abstract: | Inhibitors of histone deacetylases (HDAC) are emerging as a promising class of anti-cancer agents. A mercaptoamide functionality was designed as a bidentate zinc chelator and incorporated into the hydroxamic acid based SAHA (1) scaffold in order to identify non-hydroxamate compounds as potential inhibitors of histone deacetylases. Two sets of mercaptoamides 2 and 3 with varying spacer length were synthesized and their HDAC inhibitory activity was evaluated. Low micromolar inhibition was observed for mercaptoamides 2e, 3b, and 3d. |
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