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  • Title: Core exploration in optimization of chemokine receptor CCR4 antagonists.
    Author: Purandare AV, Wan H, Somerville JE, Burke C, Vaccaro W, Yang X, McIntyre KW, Poss MA.
    Journal: Bioorg Med Chem Lett; 2007 Feb 01; 17(3):679-82. PubMed ID: 17098428.
    Abstract:
    The design, synthesis, and SAR studies of 'core' variations led to identification of novel, selective, and potent small molecule antagonist (22) of the CC chemokine receptor-4 (CCR4) with improved in vitro activity and liability profile. Compound 22 was efficacious in a murine allergic inflammation model (ED50 approximately 10 mg/kg).
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