Article
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.
Journal of medicinal chemistry - 11 Nov 2010
Wang Xiaolun, Berger Dan M, Salaski Edward J, Torres Nancy, Dutia Minu, Hanna Cilien, Hu Yongbo, Levin Jeremy I, Powell Dennis, Wojciechowicz Donald, Collins Karen, Frommer Eileen, Lucas Judy
Abstract excerpt
Novel indazolylpyrazolo[1,5-a]pyrimidine analogues have been prepared and found to be extremely potent type I B-Raf inhibitors. The lead compound shows good selectivity against a panel of 60 kinases, possesses a desirable pharmacokinetic profile, and demonstrates excellent in vivo antitumor efficacy in B-Raf mutant xenograft models.
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