Indazolylpyrazolopyrimidine as Highly Potent B-Raf Inhibitors with in Vivo Activity
详细信息 查看全文
- 作者：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
- 刊名：Journal of Medicinal Chemistry
- 出版年：2010
- 出版时间：November 11, 2010
- 年：2010
- 卷：53
- 期：21
- 页码：7874-7878
- 全文大小：858K
- 年卷期：v.53,no.21(November 11, 2010)
- ISSN：1520-4804
文摘
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.