Core exploration in optimization of chemokine receptor CCR4 antagonists

  • Bioorg Med Chem Lett. 2007 Feb 1;17(3):679-82. doi: 10.1016/j.bmcl.2006.10.091.
Ashok V Purandare  1 ,  Honghe Wan ,  John E Somerville ,  Christine Burke ,  Wayne Vaccaro ,  XiaoXia Yang ,  Kim W McIntyre ,  Michael A Poss
Affiliations
  • 1. Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA. [email protected]
PMID: 17098428 DOI: 10.1016/j.bmcl.2006.10.091
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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