Synthesis and Biological Activity of Novel PI3K/mTOR Inhibitors

被引：2

作者：

Wang Lei ^{[1
,2
]}

Zheng Guojun ^{[1
]}

Ji Qi ^{[2
]}

Chen Bo ^{[2
]}

Gong Longlong ^{[2
]}

Gao Congmin ^{[2
]}

Du Zhenjian ^{[2
]}

Zhang Xingmin ^{[2
]}

机构：

[1] Beijing Univ Chem Technol, Coll Life Sci & Technol, Beijing 100029, Peoples R China

[2] ForelandPharma Co Ltd, Beijing 101111, Peoples R China

来源：

CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE | 2017年 / 38卷 / 09期

关键词：

Phosphatidylinositol 3-kinase/mammalian target of rapamycin(PI3K/mTOR) inhibitor; Antitumor viability; Structure-activity relationship; MTOR INHIBITORS; NVP-BEZ235; DESIGN; DERIVATIVES; DISCOVERY; PI3K;

D O I：

10.7503/cjcu20170136

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of new phosphatidylinositol 30-kinase/mammalian target of rapamycin (PI3K/mTOR) inhibitors with optimized synthetic process was designed and synthesized, the correctness of the structure was determined by H-1 NMR and LC-MS and the antitumor activities of these compounds were evaluated in 3 tumor celllines by MTT colorimetric method. Compound 11 showed very strong inhibition of MV4-11 cell growth, and was selected as a leading compound for further development of anti. leukemia drug candidate.

引用

页码：1590 / 1595

页数：6

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