Histone deacetylase inhibitors through click chemistry

J Shen, R Woodward, JP Kedenburg…

Index: Shen, Jie; Woodward, Robert; Kedenburg, James Patrick; Liu, Xianwei; Chen, Min; Fang, Lanyan; Sun, Duxin; Wang, Peng George Journal of Medicinal Chemistry, 2008 , vol. 51, # 23 p. 7417 - 7427

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Citation Number: 63

Abstract

Histone deacetylase inhibitors (HDACi) are a relatively new class of chemotherapy agents. Herein, we report a click-chemistry based approach to the synthesis of HDACi. Fourteen agents were synthesized from the combination of two alkyne and seven azido precursors. The inhibition of HDAC1 and HDAC8 was then determined by in vitro enzymatic assays, after which the cytotoxicity was evaluated in the NCI human cancer cell line screen. A lead ...

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