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  • Title: Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.
    Author: Claridge S, Raeppel F, Granger MC, Bernstein N, Saavedra O, Zhan L, Llewellyn D, Wahhab A, Deziel R, Rahil J, Beaulieu N, Nguyen H, Dupont I, Barsalou A, Beaulieu C, Chute I, Gravel S, Robert MF, Lefebvre S, Dubay M, Pascal R, Gillespie J, Jin Z, Wang J, Besterman JM, MacLeod AR, Vaisburg A.
    Journal: Bioorg Med Chem Lett; 2008 May 01; 18(9):2793-8. PubMed ID: 18434145.
    Abstract:
    A series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases is described. The compounds demonstrated potency with IC(50) 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.
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