Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity
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.
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
supporting information; scheme or table
p. 7874 - 7878
(2011/01/12)
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