趋化因子受体CCR4拮抗剂优化的核心探索
Core exploration in optimization of chemokine receptor CCR4 antagonists.
作者信息
Purandare Ashok V, Wan Honghe, Somerville John E, Burke Christine, Vaccaro Wayne, Yang XiaoXia, McIntyre Kim W, Poss Michael A
机构信息
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA.
出版信息
Bioorg Med Chem Lett. 2007 Feb 1;17(3):679-82. doi: 10.1016/j.bmcl.2006.10.091. Epub 2006 Nov 2.
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).
对“核心”结构变体的设计、合成及构效关系研究，促成了新型、选择性且强效的小分子CC趋化因子受体4（CCR4）拮抗剂（22）的鉴定，其体外活性和药物性质得到了改善。化合物22在小鼠过敏性炎症模型中有效（半数有效量约为10毫克/千克）。
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