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合成一系列新型含苯甲醚的肉桂酰衍生物作为组蛋白去乙酰化酶抑制剂。

Synthesis of a novel series of benzylether-containing cinnamoyl derivatives as histone deacetylase inhibitors.

机构信息

Department of Medicinal Chemistry, School of Pharmacy, Shan Dong University, Ji'nan, P. R. China.

出版信息

J Enzyme Inhib Med Chem. 2010 Feb;25(1):132-8. doi: 10.3109/14756360903049034.

DOI:10.3109/14756360903049034
PMID:19558346
Abstract

Histone deacetylases (HDACs) play an important role in gene transcription, cellular proliferation, apoptosis, and tumorigenesis. A novel series of benzylether-containing cinnamoyl derivatives were designed and synthesized as inhibitors of histone deacetylases (HDACs). Most of these compounds possessed inhibitory activity against the enzymes with IC50 values as low as 30 microM. In addition, compounds 4d (IC50 = 11.1 microM) and 4n (IC50 = 7.7 microM) exhibited high antiproliferative activity against tumor cell growth and effectively induced cell cycle arrest.

摘要

组蛋白去乙酰化酶（HDACs）在基因转录、细胞增殖、细胞凋亡和肿瘤发生中发挥着重要作用。设计并合成了一系列新型含苄醚的肉桂酰衍生物作为组蛋白去乙酰化酶（HDACs）的抑制剂。这些化合物大多数对酶具有抑制活性，IC50 值低至 30μM。此外，化合物 4d（IC50=11.1μM）和 4n（IC50=7.7μM）对肿瘤细胞生长具有很强的抗增殖活性，并能有效诱导细胞周期停滞。

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