| Literature DB >> 17395464 |
Douglas F Burdi1, Shannon Chi, Karen Mattia, Celeste Harrington, Zhan Shi, Shaowu Chen, Swanee Jacutin-Porte, Robert Bennett, Kenneth Carson, Wei Yin, Vikram Kansra, Jose-Angel Gonzalo, Anthony Coyle, Bruce Jaffee, Timothy Ocain, Marty Hodge, Gregory LaRosa, Geraldine Harriman.
Abstract
The identification, optimization, and structure-activity relationship (SAR) of small-molecule CCR4 antagonists is described. An initial screening hit with micromolar potency was identified that was optimized to sub-micromolar binding potency by enantiomer resolution, halogenation of the naphthalene ring, and extension of the alkyl chain linker between the central piperidine ring and the terminal aryl group. An antagonist was identified that showed good cross-reactivity against the mouse receptor and inhibited CCR4-based cell recruitment in dose-dependent fashion.Entities:
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Year: 2007 PMID： 17395464 DOI： 10.1016/j.bmcl.2007.03.030
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823