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

doi:10.1007/s40242-016-6105-7

高等学校化学研究 ›› 2016, Vol. 32 ›› Issue (4): 576-580.doi: 10.1007/s40242-016-6105-7

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

收稿日期:2016-03-23 修回日期:2016-04-27 出版日期:2016-08-01 发布日期:2016-05-30
通讯作者: LU Haibin, MU Xupeng E-mail:haibin1025@163.com;muxupeng@126.com
基金资助:
Supported by the National Natural Science Foundation of China(No.31540082).

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).

摘要/Abstract

摘要：

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.

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

Abstract:

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]. 高等学校化学研究, 2016, 32(4): 576-580.

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

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

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