Design, Synthesis, Inhibiting HDACs Ability and Antitumor Activity of Pyrimidin-4(3H)-one Hydroxamate Derivatives

doi:10.1007/s40242-016-6105-7

Chemical Research in Chinese Universities ›› 2016, Vol. 32 ›› Issue (4): 576-580.doi: 10.1007/s40242-016-6105-7

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Design, Synthesis, Inhibiting HDACs Ability and Antitumor Activity of Pyrimidin-4(3H)-one Hydroxamate Derivatives

LU Haibin¹, JIN Xiangqun¹, JIN Yang¹, HUANG Bangrui¹, WANG Cheng¹, WANG Chunhe¹, MA Fangyuan¹, CHEN Yuting¹, LI Jiarui¹, CONG Yu¹, WANG Wenlong¹, SONG Yuming², MU Xupeng²

1. College of Pharmacy, Jilin University, Changchun 130021, P. R. China;
2. China-Japan Union Hospital of Jilin University, Changchun 130033, P. R. China

Received:2016-03-23 Revised:2016-04-27 Online:2016-08-01 Published:2016-05-30
Contact: LU Haibin, MU Xupeng E-mail:haibin1025@163.com;muxupeng@126.com
Supported by:
Supported by the National Natural Science Foundation of China(No.31540082).

Abstract

Abstract:

A series of novel pyrimidin-4(3H)-one hydroxamate derivatives was designed, synthesized and studied for their activities against histone deacetylases(HDACs). The results indicate that all the compounds show HDACs inhibitiory activity. The antiproliferative activities of the compounds against HeLa and A549 cells were also investigated. The pharmacological results show compound 9g has potent activity in the enzymatic inhibition assay and cell-based assay.

Key words: Histone deacetylase, Antitumor acitivty, Pyrimidin-4(3H)-one hydroxamate derivative

LU Haibin, JIN Xiangqun, JIN Yang, HUANG Bangrui, WANG Cheng, WANG Chunhe, MA Fangyuan, CHEN Yuting, LI Jiarui, CONG Yu, WANG Wenlong, SONG Yuming, MU Xupeng. Design, Synthesis, Inhibiting HDACs Ability and Antitumor Activity of Pyrimidin-4(3H)-one Hydroxamate Derivatives[J]. Chemical Research in Chinese Universities, 2016, 32(4): 576-580.

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Design, Synthesis, Inhibiting HDACs Ability and Antitumor Activity of Pyrimidin-4(3H)-one Hydroxamate Derivatives

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