Design, synthesis and biological evaluation of acylhydrazone derivatives as PI3K inhibitors
文献类型：期刊论文
| 作者 | Gao, Guo-Rui1; Liu, Jia-Li2; Mei, De-Sheng3; Ding, Jian2 ; Meng, Ling-Hua2; Duan, Wen-Hu1,3
|
| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2015-01 |
| 卷号 | 26期号:1页码:118-120 |
| 关键词 | PI3K Inhibitor Aclhydrazone |
| ISSN号 | 1001-8417 |
| DOI | 10.1016/j.cclet.2014.10.016 |
| 文献子类 | Article |
| 英文摘要 | Since the PI3K signaling pathway is the most commonly activated in human cancers, inhibition of PI3K K 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 p110 alpha enzymatic and Rh30 cellular assays. Further enzyme selectivity profiling proved that 6e and 7 were potential selective P13K inhibitors. (C) 2014 Ling-Hua Meng and Wen-Hu Duan. Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. All rights reserved. |
| WOS关键词 | PI3-KINASE P110-ALPHA INHIBITORS ; 3-KINASE ; PATHWAY |
| 资助项目 | National Natural Science Foundation of China[81273365] ; National Natural Science Foundation of China[81321092] ; Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2012ZX09103101-024] ; Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2014ZX09304002-008-001] ; Chinese National Programs for High Technology Research and Development[2012AA020302] ; Shanghai Science and Technology Commission[11431921100] ; Shanghai Science and Technology Commission[12DZ1930802] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5349995 |
| WOS记录号 | WOS:000349577900027 |
| 出版者 | ELSEVIER SCIENCE INC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276753]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药理学第一研究室 |
| 通讯作者 | Meng, Ling-Hua |
| 作者单位 | 1.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Gao, Guo-Rui,Liu, Jia-Li,Mei, De-Sheng,et al. Design, synthesis and biological evaluation of acylhydrazone derivatives as PI3K inhibitors[J]. CHINESE CHEMICAL LETTERS,2015,26(1):118-120. |
| APA | Gao, Guo-Rui,Liu, Jia-Li,Mei, De-Sheng,Ding, Jian,Meng, Ling-Hua,&Duan, Wen-Hu.(2015).Design, synthesis and biological evaluation of acylhydrazone derivatives as PI3K inhibitors.CHINESE CHEMICAL LETTERS,26(1),118-120. |
| MLA | Gao, Guo-Rui,et al."Design, synthesis and biological evaluation of acylhydrazone derivatives as PI3K inhibitors".CHINESE CHEMICAL LETTERS 26.1(2015):118-120. |
入库方式： OAI收割
来源：上海药物研究所
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