Design and synthesis of thiazole-5-hydroxamic acids as novel histone deacetylase inhibitors

SK Anandan, JS Ward, RD Brokx, T Denny…

Index: Anandan, Sampath-Kumar; Ward, John S.; Brokx, Richard D.; Denny, Trisha; Bray, Mark R.; Patel, Dinesh V.; Xiao, Xiao-Yi Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 21 p. 5995 - 5999

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Citation Number: 29

Abstract

We have designed and synthesized a series of structurally novel hydroxamic acid-based histone deacetylase (HDAC) inhibitors characterized by a zinc chelating head group attached directly to a thiazole ring. The thiazole ring connects to a piperazine spacer, which is capped with a sulfonamide group. These novel molecules potently inhibit an HDAC enzyme mixture derived from HeLa cervical carcinoma cells and show potent ...