Design,synthesis and biological evaluation of acylhydrazone derivatives as PI3K inhibitors |
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| Authors: | Guo-Rui Gao Jia-Li Liu De-Sheng Mei Jian Ding Ling-Hua Meng Wen-Hu Duan |
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| Affiliation: | a School of Pharmacy, East China University of Science & Technology, Shanghai 200237, China;b Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;c Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China |
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| 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. |
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| Keywords: | PI3K Inhibitor Aclhydrazone |
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