Modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity

C Salmi-Smail, A Fabre, F Dequiedt…

Index: Salmi-Smail, Chanaz; Fabre, Aurelie; Dequiedt, Franck; Restouin, Audrey; Castellano, Remy; Garbit, Slaveia; Roche, Philippe; Morelli, Xavier; Brunel, Jean Michel; Collette, Yves Journal of Medicinal Chemistry, 2010 , vol. 53, # 8 p. 3038 - 3047

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Citation Number: 21

Abstract

A series of SAHA cap derivatives was designed and prepared in good-to-excellent yields that varied from 49% to 95%. These derivatives were evaluated for their antiproliferative activity in several human cancer cell lines. Antiproliferative activity was observed for concentrations varying from 0.12 to> 100 μM, and a molecular modeling approach of selected SAHA derivatives, based on available structural information of human HDAC8 in ...