Discovery and SAR of trisubstituted thiazolidinones as CCR4 antagonists

Shelley Allen; Bradley Newhouse; Aaron S Anderson; Benjamin Fauber; Andrew Allen; David Chantry; Christine Eberhardt; Joshua Odingo; Laurence E Burgess

doi:10.1016/j.bmcl.2004.01.072

Discovery and SAR of trisubstituted thiazolidinones as CCR4 antagonists

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1619-24. doi: 10.1016/j.bmcl.2004.01.072.

Authors

Shelley Allen¹, Bradley Newhouse, Aaron S Anderson, Benjamin Fauber, Andrew Allen, David Chantry, Christine Eberhardt, Joshua Odingo, Laurence E Burgess

Affiliation

¹ Array BioPharma, 3200 Walnut Street, Boulder, CO 80301, USA.

PMID: 15026036
DOI: 10.1016/j.bmcl.2004.01.072

Abstract

Substituted thiazolidinones were identified as CCR4 antagonists from high throughput screening. Subsequent lead optimization efforts resulted in defined structure-activity relationships and the identification of potent antagonists (compounds 90 and 91) that inhibited the chemotaxis of Th2 T-cells in vitro.

MeSH terms

Animals
Mice
Protein Binding / physiology
Receptors, CCR4
Receptors, Chemokine / antagonists & inhibitors*
Receptors, Chemokine / metabolism
Structure-Activity Relationship
Thiazolidinediones / chemistry*
Thiazolidinediones / metabolism
Thiazolidinediones / pharmacology

Substances

Ccr4 protein, mouse
Receptors, CCR4
Receptors, Chemokine
Thiazolidinediones