Design,synthesis and biological evaluation of acylhydrazone derivatives as PI3K inhibitors

被引：3

作者：

Guo-Rui Gao ^{[1
]}

Jia-Li Liu ^{[2
]}

De-Sheng Mei ^{[3
]}

Jian Ding ^{[2
]}

Ling-Hua Meng ^{[2
]}

Wen-Hu Duan ^{[1
,3
]}

机构：

[1] School of Pharmacy,East China University of Science & Technology

[2] Division of Anti-tumor Pharmacology,State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences

[3] Department of Medicinal Chemistry,Shanghai Institute of Materia Medica,Chinese Academy of Sciences

来源：

Chinese Chemical Letters | 2015年 / 26卷 / 01期

基金：

中国国家自然科学基金;

关键词：

PI3K; Inhibitor; Aclhydrazone;

D O I：

暂无

中图分类号：

O621.3 [有机合成化学];

学科分类号：

070303 ; 081704 ;

摘要：

Since the PI3K signaling pathway is the most commonly activated in human cancers,inhibition of PI3K is a promising approach to cancer therapy.In this study,a series of 2-methyl-5-nitrobenzeneacylhydrazones were designed and synthesized.All the new derivatives were tested by p110α enzymatic and Rh30 cellular assays.Further enzyme selectivity profiling proved that 6e and 7 were potential selective PI3K inhibitors.

引用

页码：118 / 120

页数：3

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