Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors

S Dallavalle, R Cincinelli, R Nannei, L Merlini…

Index: Dallavalle, Sabrina; Cincinelli, Raffaella; Nannei, Raffaella; Merlini, Lucio; Morini, Gabriella; Penco, Sergio; Pisano, Claudio; Vesci, Loredana; Barbarino, Marcella; Zuco, Valentina; De Cesare, Michelandrea; Zunino, Franco European Journal of Medicinal Chemistry, 2009 , vol. 44, # 5 p. 1900 - 1912

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Citation Number: 52

Abstract

A series of hydroxamic acid-based histone deacetylase (HDAC) inhibitors were designed on the basis of a model of the HDAC2 binding site and synthesized. They are characterized by a cinnamic spacer, capped with a substituted phenyl group. Modifications of the spacer are also reported. In an in vitro assay with the isoenzyme HDAC2, a good correlation of the activity with the docking energy was found. In human ovarian carcinoma IGROV-1 cells, ...