Literature DB >> 19131247

Discovery of trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.

Robert J Cherney1, John B Brogan, Ruowei Mo, Yvonne C Lo, Gengjie Yang, Persymphonie B Miller, Peggy A Scherle, Bruce F Molino, Percy H Carter, Carl P Decicco.   

Abstract

A series of trisubstituted cyclohexanes was designed, synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. This led to the identification of two distinct substitution patterns about the cyclohexane ring as potent and selective CCR2 antagonists. Compound 36 exhibited excellent binding (CCR2 IC(50)=2.4 nM) and functional antagonism (calcium flux IC(50)=2.0 nM and chemotaxis IC(50)=5.1 nM).

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Year:  2008        PMID: 19131247     DOI: 10.1016/j.bmcl.2008.12.062

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Hydroxyl Groups on Annular Ring-B Dictate the Affinities of Flavonol-CCL2 Chemokine Binding Interactions.

Authors:  Nidhi Joshi; Deepak Kumar Tripathi; Nupur Nagar; Krishna Mohan Poluri
Journal:  ACS Omega       Date:  2021-04-06

2.  Targeting the androgen receptor with siRNA promotes prostate cancer metastasis through enhanced macrophage recruitment via CCL2/CCR2-induced STAT3 activation.

Authors:  Kouji Izumi; Lei-Ya Fang; Atsushi Mizokami; Mikio Namiki; Lei Li; Wen-Jye Lin; Chawnshang Chang
Journal:  EMBO Mol Med       Date:  2013-08-27       Impact factor: 12.137

  2 in total

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