Design and synthesis of aryl ether and sulfone hydroxamic acids as potent histone deacetylase (HDAC) inhibitors

…, BT Gregg, DB Kitchen, ZJ Chen, A Judkins

Index: Pabba, Chittari; Gregg, Brian T.; Kitchen, Douglas B.; Chen, Zhen Jia; Judkins, Angela Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 324 - 328

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Citation Number: 13

Abstract

A series of novel hydroxamic acid based histone deacetylases (HDAC) inhibitors with aryl ether and aryl sulfone residues at the terminus of a substituted, unsaturated 5-carbon spacer moiety have been synthesized for the first time and evaluated. Compounds with meta-and para-substitution on the aryl ring of ether hydroxamic acids 19c, 20c, 19e, 19f and 19g are potent HDAC inhibitors with activities at low nanomolar levels.

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