中国科学院机构知识库网格系统: Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold

Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold

文献类型：期刊论文


作者	Zhao, Ailing 2; Gao, Xin 1; Wang, Yuanxiang 2; Ai, Jing1 ; Wang, Ying 1; Chen, Yi1 ; Geng, Meiyu1 ; Zhang, Ao2
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
出版日期	2011-07-01
卷号	19 期号:13 页码:3906-3918
关键词	RTK c-Met Thieno[2,3-d]pyrimidine Furo[2,3-d]pyrimidine Antitumor
ISSN号	0968-0896
DOI	10.1016/j.bmc.2011.05.038
文献子类	Article
英文摘要	A series of thieno[2,3-d]pyrimidines and furo[2,3-d] pyrimidines were synthesized and evaluated for the c-Met inhibition. Thieno[2,3-d]pyrimidine 6b stood out as the most potent showing an IC(50) of 35.7 nM. This compound displayed high inhibitory effect on cell proliferation in BaF3-TPR-Met cells and showed high selectivity for c-Met family against other 14 tested kinases. However, compound 6b was found ineffective in the c-Met-dependent U-87MG human gliobastoma xenograft model that may be relevant to its poor PK profile. (C) 2011 Elsevier Ltd. All rights
WOS关键词	FACTOR SCATTER FACTOR ; TYROSINE KINASE ; BIOLOGICAL EVALUATION ; SELECTIVE INHIBITORS ; GROWTH ; POTENT ; PHENOTYPE ; CELLS ; IDENTIFICATION ; METASTASIS
资助项目	Shanghai Commission of Science and Technology[10JC1417100] ; National Science & Technology Major Project[2009ZX09301-001] ; National Science & Technology Major Project[2009ZX09103-062] ; Natural Science Foundation of China[30725046] ; Program of Shanghai Subject Chief Scientist[10XD1405100]
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种	英语
WOS记录号	WOS:000291934700004
出版者	PERGAMON-ELSEVIER SCIENCE LTD
源URL	[http://119.78.100.183/handle/2S10ELR8/278488]
专题	药理学第一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物化学研究室
通讯作者	Geng, Meiyu
作者单位	1.Chinese Acad Sci, SIMM, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, SIMM, State Key Lab Drug Res, SOMCL, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Zhao, Ailing,Gao, Xin,Wang, Yuanxiang,et al. Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(13):3906-3918.
APA	Zhao, Ailing.,Gao, Xin.,Wang, Yuanxiang.,Ai, Jing.,Wang, Ying.,...&Zhang, Ao.(2011).Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.BIOORGANIC & MEDICINAL CHEMISTRY,19(13),3906-3918.
MLA	Zhao, Ailing,et al."Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold".BIOORGANIC & MEDICINAL CHEMISTRY 19.13(2011):3906-3918.

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来源：上海药物研究所

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Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold

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