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

注册 English

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

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

Citation: Guo-Rui Gao, Jia-Li Liu, De-Sheng Mei, Jian Ding, Ling-Hua Meng, Wen-Hu Duan. Design, synthesis and biological evaluation of acylhydrazone derivatives as PI3K inhibitors[J]. Chinese Chemical Letters, 2015, 26(1): 118-120. doi: 10.1016/j.cclet.2014.10.016 shu

shu

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

通讯作者: Ling-Hua Meng,
Wen-Hu Duan,

基金项目:

Development (No. 2012AA020302) (No. 2012AA020302)

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.

关键词:

PI3K
/ Inhibitor
/ Aclhydrazone

English

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

1.
a School of Pharmacy, East China University of Science & Technology, Shanghai 200237, China;
2.
b Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;
3.
c Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China

Corresponding author: Ling-Hua Meng, Wen-Hu Duan,

Received Date: 11 July 2014
Available Online: 01 November 2014

Abstract: 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.

Key words:

PI3K
/ Inhibitor
/ Aclhydrazone

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