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

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

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

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: 14 October 2014
Fund Project:

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.
- PI3K,
- Inhibitor,
- Aclhydrazone
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