An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFR? and kit.
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ABSTRACT:
SUBMITTER: Deng X
PROVIDER: S-EPMC3547541 | biostudies-literature | 2012 Jul
REPOSITORIES: biostudies-literature
Publications
An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRα and kit.
Deng Xianming X Zhou Wenjun W Weisberg Ellen E Wang Jinhua J Zhang Jianming J Sasaki Takaaki T Nelson Erik E Griffin James D JD Jänne Pasi A PA Gray Nathanael S NS
Bioorganic & medicinal chemistry letters 20120606 14
Here we describe the synthesis and characterization of a number of 3-amino-1H-indazol-6-yl-benzamides that were designed to target the 'DFG-out' conformation of the kinase activation loop. Several compounds such as 4 and 11 exhibit single-digit nanomolar EC(50)s against FLT3, c-Kit and the gatekeeper T674M mutant of PDGFRα. ...[more]
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