| Literature DB >> 17350837 |
Brian L Hodous1, Stephanie D Geuns-Meyer, Paul E Hughes, Brian K Albrecht, Steve Bellon, Sean Caenepeel, Victor J Cee, Stuart C Chaffee, Maurice Emery, Jenne Fretland, Paul Gallant, Yan Gu, Rebecca E Johnson, Joseph L Kim, Alexander M Long, Michael Morrison, Philip R Olivieri, Vinod F Patel, Anthony Polverino, Paul Rose, Ling Wang, Huilin Zhao.
Abstract
A novel class of selective Tie-2 inhibitors was derived from a multi-kinase inhibitor 1. By reversing the amide connectivity and incorporating aminotriazine or aminopyridine hinge-binding moieties, excellent Tie-2 potency and KDR selectivity could be achieved with 3-substituted terminal aryl rings. X-ray co-crystal structure analysis aided inhibitor design. This series was evaluated on the basis of potency, selectivity, and rat pharmacokinetic parameters.Entities:
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Year: 2007 PMID： 17350837 DOI： 10.1016/j.bmcl.2007.02.067
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823