Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors

doi:10.1021/acsmedchemlett.6b00066

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	Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors
	Zhao, Bin 2; Li, Yixuan 3; Xu, Pan 1; Dai, Yang 3; Luo, Cheng1 ; Sun, Yiming 3; Ai, Jing3 ; Geng, Meiyu3 ; Duan, Wenhu2
刊名	ACS MEDICINAL CHEMISTRY LETTERS
	2016-06
卷号	7 期号:6 页码:629-634
关键词	Cancer FGFR inhibitor pyrazolo[3,4-b]pyridine
ISSN号	1948-5875
DOI	10.1021/acsmedchemlett.6b00066
文献子类	Article
英文摘要	Fibroblast growth factor receptors (FGFRs) are important targets for cancer therapy. Herein, we describe the design, synthesis, and biological evaluation of a novel series of 1H-pyrazolo[3,4-b]pyridine derivatives as potent and selective FGFR kinase inhibitors. On the basis of its excellent in vitro potency and favorable pharmacokinetic properties, compound 7n was selected for in vivo evaluation and showed significant antitumor activity in a FGFR1-driven H1581 xenograft model. These results indicated that 7n would be a promising candidate for further drug development.
资助项目	National Natural Science Foundation of China[81273365] ; National Natural Science Foundation of China[81573271] ; National Natural Science Foundation of China[81473243] ; National Natural Science Foundation of China[81321092] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2014ZX09304002-008-001] ; Shanghai Science and Technology Commission[1315431901300]
WOS关键词	RECEPTOR TYROSINE KINASE ; CANCER ; ANGIOGENESIS ; MANAGEMENT ; FAMILY
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000377845200018
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276019]
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	Ai, Jing; Geng, Meiyu; Duan, Wenhu
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Dept Med Chem, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China;
推荐引用方式 GB/T 7714	Zhao, Bin,Li, Yixuan,Xu, Pan,et al. Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors[J]. ACS MEDICINAL CHEMISTRY LETTERS,2016,7(6):629-634.
APA	Zhao, Bin.,Li, Yixuan.,Xu, Pan.,Dai, Yang.,Luo, Cheng.,...&Duan, Wenhu.(2016).Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors.ACS MEDICINAL CHEMISTRY LETTERS,7(6),629-634.
MLA	Zhao, Bin,et al."Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors".ACS MEDICINAL CHEMISTRY LETTERS 7.6(2016):629-634.