Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of …

…, G Brosch, P Loidl, C Gerhäuser, M Jung

Index: Jung, Manfred; Brosch, Gerald; Koelle, Doris; Scherf, Hans; Gerhaeuser, Clarissa; Loidl, Peter Journal of Medicinal Chemistry, 1999 , vol. 42, # 22 p. 4669 - 4679

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Citation Number: 87

Abstract

Inhibitors of histone deacetylases (HDACs) are a new class of anticancer agents that affect gene regulation. We had previously reported the first simple synthetic HDAC inhibitors with in vitro activity at submicromolar concentrations. Here, we present structure-activity data on modifications of a phenylalanine-containing lead compound including amino acid amides as well as variations of the amino acid part. The compounds were tested for inhibition of ...

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