| Literature DB >> 19854647 |
Richard W A Luke1, Peter Ballard, David Buttar, Leonie Campbell, Jon Curwen, Steve C Emery, Alison M Griffen, Lorraine Hassall, Barry R Hayter, Cliff D Jones, William McCoull, Martine Mellor, Mike L Swain, Julie A Tucker.
Abstract
The SAR and improvement in potency against Tie2 of novel thienopyrimidine and thiazolopyrimidine kinase inhibitors are reported. The crystal structure of one of these compounds bound to the Tie-2 kinase domain is consistent with the SAR. These compounds have moderate potency in cellular assays of Tie-2 inhibition, good physical properties, DMPK, and show evidence of in vivo inhibition of Tie-2.Entities:
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Year: 2009 PMID： 19854647 DOI： 10.1016/j.bmcl.2009.10.001
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823