Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases

Authors:	Claridge Stephen Raeppel Franck Granger Marie-Claude Bernstein Naomy Saavedra Oscar Zhan Lijie Llewellyn David Wahhab Amal Deziel Robert Rahil Jubrail Beaulieu Normand Nguyen Hannah Dupont Isabelle Barsalou Annie Beaulieu Carole Chute Ian Gravel Serge Robert Marie-France Lefebvre Sylvain Dubay Marja Pascal Roussen Gillespie Jeff Jin Zhiyun Wang James Besterman Jeffrey M MacLeod A Robert Vaisburg Arkadii

Institution:	^aDepartment of Medicinal Chemistry, MethylGene Inc., 7220 Frederick-Banting, Montréal, Que., Canada H4S 2A1 ^bDepartment of Cell Biology and Pharmacology, MethylGene Inc., 7220 Frederick-Banting, Montréal, Que., Canada H4S 2A1 ^cDepartment of Lead Discovery, MethylGene Inc., 7220 Frederick-Banting, Montréal, Que., Canada H4S 2A1 ^dDepartment of PK/Analytical Chemistry, MethylGene Inc., 7220 Frederick-Banting, Montréal, Que., Canada H4S 2A1

Abstract:	A series of thieno3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases is described. The compounds demonstrated potency with IC₅₀ values in the low nanomolar range in vitro while the lead compound also showed in vivo activity against various human tumor xenograft models in mice. Further exploration of this class of compounds is underway.

Keywords:	c-Met VEGFR2 Kinase Thieno[3 2-b]pyridine Cancer
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