Format

Send to:

Choose Destination
See comment in PubMed Commons below
Bioorg Med Chem Lett. 2012 Jun 15;22(12):4089-93. doi: 10.1016/j.bmcl.2012.04.072. Epub 2012 Apr 25.

Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.

Author information

  • 1Amgen Inc., 360 Binney St., Cambridge, MA 02142, USA. aboezio@amgen.com

Abstract

Deregulation of the receptor tyrosine kinase c-Met has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, we report the discovery of a structurally diverse series of carbon-linked quinoline triazolopyridinones, which demonstrates nanomolar inhibition of c-Met kinase activity. This novel series of inhibitors exhibits favorable pharmacokinetics as well as potent inhibition of HGF-mediated c-Met phosphorylation in a mouse liver pharmacodynamic model.

Copyright © 2012 Elsevier Ltd. All rights reserved.

PMID:
22595176
[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Write to the Help Desk