| Literature DB >> 16621534 |
Thomas D Penning1, Albert Khilevich, Barbara B Chen, Mark A Russell, Mark L Boys, Yaping Wang, Tiffany Duffin, V Wayne Engleman, Mary Beth Finn, Sandra K Freeman, Melanie L Hanneke, Jeffery L Keene, Jon A Klover, G Allen Nickols, Maureen A Nickols, Randall K Rader, Steven L Settle, Kristen E Shannon, Christina N Steininger, Marisa M Westlin, William F Westlin.
Abstract
We describe a series of pyrazole and isoxazole analogs as antagonists of the alpha(v)beta3 receptor. Compounds showed low to sub-nanomolar potency against alpha(v)beta3, as well as good selectivity against alpha(IIb)beta3. In HT29 cells, most analogs also demonstrated significant selectivity against alpha(v)beta6. Several compounds showed good pharmacokinetic properties in rats, in addition to anti-angiogenic activity in a mouse corneal micropocket model. Compounds were synthesized in a straightforward manner from readily available glutarate precursors.Entities:
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Year: 2006 PMID： 16621534 DOI： 10.1016/j.bmcl.2006.03.045
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823