In an effort to obtain more information on the structure-activity relationship among the 7 alpha-(phenylthio)androstenedione inhibitors of the enzyme aromatase, a series of compounds containing both electron-donating and electron-withdrawing ring substituents was synthesized and tested for aromatase inhibitory activity. No linear correlation between substituent electronic effects and inhibitory activity
为了获得有关7种芳香酶的α-(苯
硫基)
雄烯二酮抑制剂之间的构效关系的更多信息,合成了一系列同时具有给电子和吸电子环取代基的化合物,并测试了其对芳香酶的抑制作用。活动。在取代基电子效应和抑制活性之间没有观察到线性相关性。含卤素的化合物,特别是8种,似乎是非常有效的
抑制剂。为了评估在测定条件下消除侧链的可能性,合成了8的125I类似物。在测定条件下,大约90%的[125I] -8保持完整状态长达1小时。