Antiproliferative activities of a library of hybrids between indanones and HDAC inhibitor SAHA and MS-275 analogues

被引:16
作者
Charrier, Cedric
Roche, Joeelle
Gesson, Jean-Pierre
Bertrand, Philippe
机构
[1] Univ Poitiers, CNRS UMR 6514, Synth React Subst Nat, F-86022 Poitiers, France
[2] Univ Poitiers, CNRS UMR 6187, Inst Physiol Biol Cellular, F-86022 Poitiers, France
关键词
historic deacetylase; cancer; epigenetic; trichostatin A; SAHA; MS-275; indanones; hybrid;
D O I
10.1016/j.bmcl.2007.09.041
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
New compounds derived from inhibitors of histone deacetylases (HDACs) have been synthesized and their antiproliferative activities towards non small lung cancer cell line H661 evaluated. Their design is based on hybrids between indanones to limit conformational mobility and other known HDAC inhibitors (SAHA, MS-275). The synthesis of these new derivatives was achieved by alkylation of appropriate indanones to introduce the side chain bearing a terminal ester group, the latter being a precursor of hydroxamic acid and aminobenzamide derivatives. These new analogues were found to be moderately active to inhibit H661 cell proliferation. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6142 / 6146
页数:5
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