Structure-activity relationships of indole cytosolic phospholipase A(2)alpha inhibitors: substrate mimetics
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...
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Published in | Bioorganic & medicinal chemistry letters Vol. 13; no. 24; pp. 4501 - 4504 |
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Main Authors | , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
England
15.12.2003
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Subjects | |
Online Access | Get full text |
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Summary: | 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. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0960-894X |
DOI: | 10.1016/j.bmcl.2003.08.070 |