Bioorganic and Medicinal Chemistry Letters, volume 19, issue 23, pages 6571-6574

Discovery of highly potent and selective type I B-Raf kinase inhibitors

Xiaolun Wang 1
, 
Dan M Berger 1
, 
Edward J. Salaski 1
, 
Nancy Torres 1
, 
Yongbo Hu 1
, 
Jeremy I Levin 1
, 
Dennis Powell 1
, 
Donald Wojciechowicz 2
, 
Karen Scott Collins 2
, 
Eileen Frommer 2
Show full list: 10 authors
1
 
Chemical Sciences, Wyeth Research, 401 N. Middletown Road., Pearl River, NY 10965, USA | 
2
 
Discovery Oncology, Wyeth Research, 401 N. Middletown Road., Pearl River, NY 10965, USA | 
Publication type: Journal Article
Publication date: 2009-12-01
scimago Q2
wos Q2
SJR: 0.508
CiteScore: 5.7
Impact factor: 2.5
ISSN: 0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
A series of pyrazolo[1,5-alpha]pyrimidine analogs has been prepared and found to be potent and selective B-Raf inhibitors. Molecular modeling suggests they bind to the active conformation of the enzyme.
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