Synthesis and Biological Activity of Imidazo[4,5-c]quinoline Derivatives as PI3K/mTOR Inhibitors

被引：5

作者：

Li Yanjie ^{[1
,2
]}

Zhang Xingmin ^{[3
]}

Niu Shengxiu ^{[1
]}

Zhao Yanping ^{[1
]}

Yang Lijuan ^{[1
]}

Shao Xiaowei ^{[1
]}

Wang Ensi ^{[1
]}

机构：

[1] Jilin Univ, Coll Pharm, Changchun 130021, Jilin, Peoples R China

[2] Changchun Univ Tradit Chinese Med, Coll Pharm, Changchun 130117, Jilin, Peoples R China

[3] Beijing Foreland Pharma Biol Technol Co Ltd, Beijing 101111, Peoples R China

来源：

CHEMICAL RESEARCH IN CHINESE UNIVERSITIES | 2017年 / 33卷 / 06期

关键词：

Imninzo[4,5-c]quinoline; Suzuki reaction; Dual PI3K/mTOR inhibitor; NVP-BEZ235; TARGET; MUTATIONS; RAPAMYCIN; GROWTH; CANCER;

D O I：

10.1007/s40242-017-7074-1

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of imidazo[4,5-c]quinoline derivatives(12a-12m) was synthesized with 2-amino-5-bromobenzoic acid and 4-nitrophenylacetonitrile as starting materials, 6-bromo-4-chloro-3-nitroquinoline as intermediate and Suzuki reaction and closure of the imidazolinone ring with triphosgene as key steps. The structures of the key intermediate and target compounds were confirmed by means of H-1-INMR, C-13 NMR and HRMS. These compounds show an interesting kinase profile as dual PI3K/mTOR tool compounds.

引用

页码：895 / 902

页数：8

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