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Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.

Abstract：

:A new series of quinoline ether inhibitors, which potently and selectively inhibit PDGFR tyrosine kinases, is described in this Letter. Compounds 23 and 33 are selective, low nanomolar inhibitors of PDGFRα and β, display good pharmacokinetics in rat and dog and are active in vivo at low doses when given orally twice daily. Further evaluation of these compounds is warranted.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Plé PA,Jung F,Ashton S,Hennequin L,Laine R,Lambert-van der Brempt C,Morgentin R,Pasquet G,Taylor S

doi

10.1016/j.bmcl.2012.03.074

subject

Has Abstract

pub_date

2012-05-01 00:00:00

pages

3050-5

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00395-2

journal_volume

22

pub_type

杂志文章

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