Mitchell Lorna H, Hu Lain-Yen, Nguyen Maria, Fakhoury Stephen, Smith Yvonne, Iula Donna, Kostlan Catherine, Carroll Matthew, Dettling Danielle, Du Daniel, Pocalyko David, Wade Kimberly, Lefker Bruce
Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, UK.
Bioorg Med Chem Lett. 2009 Apr 15;19(8):2176-8. doi: 10.1016/j.bmcl.2009.02.104. Epub 2009 Mar 3.
A series of diphenyl ethers was prepared and evaluated for androgen receptor antagonist activity in human androgen receptor binding and cellular functional assays. Analogs with potent in vitro activities were evaluated for topical in vivo efficacy in the Golden Syrian Hamster ear model. Several compounds showed reduction in wax esters in this validated animal model.
制备了一系列二苯醚，并在人雄激素受体结合和细胞功能试验中评估其雄激素受体拮抗剂活性。对具有强大体外活性的类似物在金黄叙利亚仓鼠耳部模型中进行了局部体内疗效评估。在这个经过验证的动物模型中，几种化合物显示出蜡酯减少。
