Indazolylpyrazolopyrimidine as Highly Potent B-Raf Inhibitors with in Vivo Activity
Journal of Medicinal Chemistry2010Vol. 53(21), pp. 7874–7878
Citations Over TimeTop 20% of 2010 papers
Xiaolun Wang, Dan M. Berger, Edward J. Salaski, Nancy Torres, Minu Dutia, Cilien Hanna, Yongbo Hu, Jeremy I. Levin, Dennis Powell, Donald Wojciechowicz, Karen Collins, Eileen Frommer, Judy Lucas
Abstract
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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