1258930-31-2Relevant academic research and scientific papers
Novel sulfone-containing di- and trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists
Cherney, Robert J.,Mo, Ruowei,Meyer, Dayton T.,Voss, Matthew E.,Lo, Yvonne C.,Yang, Gengjie,Miller, Persymphonie B.,Scherle, Peggy A.,Tebben, Andrew J.,Carter, Percy H.,Decicco, Carl P.
, p. 3418 - 3422 (2009)
Potent sulfone-containing di- and trisubstituted cyclohexanes were synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. This led to the trisubstituted derivative 54, which exhibited excellent binding (CCR2 IC50 = 1.3 nM) and functional antagonism (calcium flux IC50 = 0.5 nM and chemotaxis IC50 = 0.2 nM). The superiority of the trisubstituted scaffold was rationalized to be the result of a conformational rigidification, which provided insight into the bioactive conformation of this chemotype.
