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Bioorg Med Chem Lett. 2011 Sep 15;21(18):5224-9. doi: 10.1016/j.bmcl.2011.07.047. Epub 2011 Jul 23.

The discovery of benzanilides as c-Met receptor tyrosine kinase inhibitors by a directed screening approach.

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  • 1AstraZeneca R&D, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.


A directed screen of a relatively small number of compounds, selected for kinase ATP pocket binding potential, yielded a novel series of hit compounds (1). Hit explosion on two binding residues identified compounds 27 and 43 as the best leads for an optimization program having reduced secondary metabolism, as measured by in vitro rat hepatocytes incubation, leading to oral bio-availability. Structure-activity relationships and molecular modeling have suggested a binding mode for the most potent inhibitor 12.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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