3-(4-Aroyl-1 H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors

…, M Esposito, R Ragno, P Loidl, G Brosch

文献索引：Massa; Mai; Sbardella; Esposito; Ragno; Loidl; Brosch Journal of Medicinal Chemistry, 2001 , vol. 44, # 13 p. 2069 - 2072

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被引用次数: 86

摘要

Novel 3-(4-aroyl-2-pyrrolyl)-N-hydroxy-2-propenamides are disclosed as a new class of histone deacetylase (HDAC) inhibitors. Three-dimensional structure-based drug design and conformational analyses into the histone deacetylase-like protein (HDLP) catalytic core suggested the synthesis and biological evaluation of compounds 7a-h. Experimental p K i values are in good agreement with VALIDATE predicted p K i values of new derivatives. ...