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Design and Optimization of a Series of 1-Sulfonylpyrazolo[4,3-b]pyridines as Selective c-Met Inhibitors

文献类型：期刊论文

作者Ma, Yuchi1; Sun, Guangqiang2; Chen, Danqi1; Peng, Xia2; Chen, Yue-Lei1; Su, Yi2; Ji, Yinchun2; Liang, Jin1; Wang, Xin1; Chen, Lin1
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2015-03-12
卷号58期号:5页码:2513-2529
ISSN号0022-2623
DOI10.1021/jm502018y
文献子类Article
英文摘要c-Met has emerged as an attractive target for targeted cancer therapy because of its abnormal activation in many cancer cells. To identify high potent and selective c-Met inhibitors, we started with profiling the potency and in vitro metabolic stability of a reported hit 7. By rational design, a novel sulfonylpyrazolo[4,3-b]pyridine 9 with improved DMPK properties was discovered. Further elaboration of pi-pi stacking interactions and solvent accessible polar moieties led to a series of highly potent and selective type I c-Met inhibitors. On the basis of in vitro and in vivo pharmacological and pharmacokinetics studies, compound 46 was selected as a preclinical candidate for further anticancer drug development.
WOS关键词RECEPTOR TYROSINE KINASE ; SMALL-MOLECULE INHIBITOR ; ANTITUMOR-ACTIVITY ; COLORECTAL-CANCER ; INVASIVE GROWTH ; METASTASIS ; ONCOGENE ; OVEREXPRESSION ; PROTOONCOGENE ; AMPLIFICATION
资助项目"Interdisciplinary Cooperation Team" Program for Science and Technology Innovation of the Chinese Academy of Sciences[00000000] ; National Natural Science Foundation of China[81202391] ; National Natural Science Foundation of China[91229205] ; National Natural Science Foundation of China[81473243] ; National Natural Science Foundation of China[81321092] ; National Natural Science Foundation of China[81330076] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program" of China[2014ZX09507002] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program" of China[2012ZX09301001-007] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program" of China[2013ZX09507001] ; National Program on Key Basic Research Project of China[2012CB10704]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000351186500034
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/276605]  
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Xiong, Bing
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Dept Med Chem, Shanghai 201203, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Ma, Yuchi,Sun, Guangqiang,Chen, Danqi,et al. Design and Optimization of a Series of 1-Sulfonylpyrazolo[4,3-b]pyridines as Selective c-Met Inhibitors[J]. JOURNAL OF MEDICINAL CHEMISTRY,2015,58(5):2513-2529.
APA Ma, Yuchi.,Sun, Guangqiang.,Chen, Danqi.,Peng, Xia.,Chen, Yue-Lei.,...&Shen, Jingkang.(2015).Design and Optimization of a Series of 1-Sulfonylpyrazolo[4,3-b]pyridines as Selective c-Met Inhibitors.JOURNAL OF MEDICINAL CHEMISTRY,58(5),2513-2529.
MLA Ma, Yuchi,et al."Design and Optimization of a Series of 1-Sulfonylpyrazolo[4,3-b]pyridines as Selective c-Met Inhibitors".JOURNAL OF MEDICINAL CHEMISTRY 58.5(2015):2513-2529.

入库方式： OAI收割

来源：上海药物研究所

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