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Bioorg Med Chem Lett. 2012 May 1;22(9):3050-5. doi: 10.1016/j.bmcl.2012.03.074. Epub 2012 Mar 28.

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

Author information

1
AstraZeneca, Centre de Recherches, BP 1050, 51689 Reims Cedex 2, France. patrick.ple@astrazeneca.com

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.

PMID:
22497760
DOI:
10.1016/j.bmcl.2012.03.074
[Indexed for MEDLINE]

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