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

Author: Jiao Jie   Fang Hao   Wang Xuejian   Zhu Huawei   Jiang Lan   Xu Wenfang  

Publisher: Informa Healthcare

ISSN: 1475-6366

Source: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol.25, Iss.1, 2010-01, pp. : 132-138

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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 μM. In addition, compounds 4d (IC50 = 11.1 μM) and 4n (IC50 = 7.7 μM) exhibited high antiproliferative activity against tumor cell growth and effectively induced cell cycle arrest.

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