| Literature DB >> 14643356 |
John C McKew1, Frank Lovering, James D Clark, Jean Bemis, YiBin Xiang, Marina Shen, Wen Zhang, Juan C Alvarez, Diane Joseph-McCarthy.
Abstract
An SAR effort focused on generating cPLA(2)alpha inhibitors using a substrate mimetic approach is reported. Indole inhibitors of cPLA(2)alpha with promising pharmacokinetic parameters that were active in both an isolated enzyme assay and in cell-based assays were discovered. Modeling these compounds into the cPLA(2)alpha structure validated the assumptions made at the start of the SAR effort.Entities:
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Year: 2003 PMID： 14643356 DOI： 10.1016/j.bmcl.2003.08.070
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823