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

S Claridge, F Raeppel, MC Granger, N Bernstein…

文献索引：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 Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 9 p. 2793 - 2798

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被引用次数: 40

摘要

A series of thieno [3, 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.