Literature DB >> 17088058

Diaryl substituted pyrazoles as potent CCR2 receptor antagonists.

Anthony B Pinkerton1, Dehua Huang, Rowena V Cube, John H Hutchinson, Mary Struthers, Julia M Ayala, Pasquale P Vicario, Sima R Patel, Thomas Wisniewski, Julie A DeMartino, Jean-Michel Vernier.   

Abstract

We have identified and synthesized a series of diaryl substituted pyrazoles as potent antagonists of the chemokine receptor subtype 2. Structure-activity relationship studies directed toward improving the potency led to the discovery of 23 (IC50 = 6 nM).

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Year:  2006        PMID: 17088058     DOI: 10.1016/j.bmcl.2006.10.060

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


  4 in total

Review 1.  Controlled microwave heating in modern organic synthesis: highlights from the 2004-2008 literature.

Authors:  C Oliver Kappe; Doris Dallinger
Journal:  Mol Divers       Date:  2009-04-21       Impact factor: 2.943

2.  Binding site characterization of G protein-coupled receptor by alanine-scanning mutagenesis using molecular dynamics and binding free energy approach: application to C-C chemokine receptor-2 (CCR2).

Authors:  Swapnil Chavan; Shirishkumar Pawar; Rajesh Singh; M Elizabeth Sobhia
Journal:  Mol Divers       Date:  2012-04-22       Impact factor: 2.943

3.  Structural insights from binding poses of CCR2 and CCR5 with clinically important antagonists: a combined in silico study.

Authors:  Gugan Kothandan; Changdev G Gadhe; Seung Joo Cho
Journal:  PLoS One       Date:  2012-03-27       Impact factor: 3.240

4.  The CCR2/MCP-1 Chemokine Pathway and Lung Adenocarcinoma.

Authors:  Payal Mittal; Liqing Wang; Tatiana Akimova; Craig A Leach; Jose C Clemente; Matthew R Sender; Yao Chen; Brandon J Turunen; Wayne W Hancock
Journal:  Cancers (Basel)       Date:  2020-12-11       Impact factor: 6.639

  4 in total

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