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

作　　者：Guo-Rui Gao Jia-Li Liu De-Sheng Mei Jian Ding Ling-Hua Meng Wen-Hu Duan 

机构地区：[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

出　　处：《Chinese Chemical Letters》2015年第1期118-120,共3页中国化学快报（英文版）

基　　金：the National Natural Science Foundation of China(Nos.81273365 and 81321092);Chinese National Science&Technology Major Project "Key New Drug Creation and Manufacturing Program"(Nos.2012ZX09103101-024 and 2014ZX09304002-008-001);Chinese National Programs for High Technology Research and Development(No.2012AA020302);the Shanghai Science and Technology Commission(Nos.11431921100 and 12DZ1930802)for their financial support

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.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.

关 键 词：PI3K INHIBITOR Aclhydrazone 

分 类 号：O621.3[理学—有机化学]