Benzo [b] thiophene-based histone deacetylase inhibitors

…, S Belvedere, L Chen, JP Secrist, RT Mosley…

Index: Witter, David J.; Belvedere, Sandro; Chen, Liqiang; Secrist, J. Paul; Mosley, Ralph T.; Miller, Thomas A. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 16 p. 4562 - 4567

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Citation Number: 34

Abstract

Benzo [b] thienyl hydroxamic acids, a novel class of histone deacetylase (HDAC) inhibitors, were identified via a targeted screen of small molecule hydroxamic acids. Various substitutions were explored in the C5-and C6-positions of the benzo [b] thiophene core to characterize SAR and develop optimal inhibitors. It was determined that substitution at the C6-position of the benzo [b] thiophene core with a three-atom spacer yielded optimal ...