| Literature DB >> 21277198 |
Yuefei Shao1, Gopinadhan N Anilkumar, Carolyn Diianni Carroll, Guizhen Dong, James W Hall, Doug W Hobbs, Yueheng Jiang, Chung-Her Jenh, Seong Heon Kim, Joseph A Kozlowski, Brian F McGuinness, Stuart B Rosenblum, Inna Schulman, Neng-Yang Shih, Youheng Shu, Michael K C Wong, Wensheng Yu, Lisa Guise Zawacki, Qingbei Zeng.
Abstract
The structure-human CXCR3 binding affinity relationship of a series of pyridyl-piperazinyl-piperidine derivatives was explored. The optimization campaign highlighted the pronounced effect of 2'-piperazine substitution on CXCR3 receptor affinity. Analog 18j, harboring a 2'(S)-ethylpiperazine moiety, exhibited a human CXCR3 IC(50) of 0.2 nM.Entities:
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Year: 2010 PMID： 21277198 DOI： 10.1016/j.bmcl.2010.12.114
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823