Canceill J, Jacques J, Bouton M M, Fortin M, Tournemine C
J Steroid Biochem. 1983 Jun;18(6):643-7. doi: 10.1016/0022-4731(83)90241-8.
The interactions of A-nor-5 alpha-androstane and A-nor-5 alpha-estrane derivatives with the estrogen and androgen receptors, have been evaluated by measuring their relative binding affinities (RBAs), under two sets of incubation conditions in order to discriminate between potent agonists from weak agonists with potential antagonist activities. Surprisingly some of these compounds which do not possess a phenolic hydroxyl group interact somewhat markedly with the estrogen receptor. This interaction is characteristic of weak estrogens, with potential anti-estrogenic activity (RBA values decreasing when increasing time and temperature of incubation). Results are in good agreement with data obtained in vivo. Moreover, some of these compounds interact also to some extent with the androgen receptor. Results will be discussed in order to outline some structure-activity relationships in these series.
通过测量其相对结合亲和力（RBAs），在两组孵育条件下评估了A-去甲-5α-雄甾烷和A-去甲-5α-雌甾烷衍生物与雌激素和雄激素受体的相互作用，以便区分具有潜在拮抗活性的强效激动剂和弱激动剂。令人惊讶的是，这些不具有酚羟基的化合物中的一些与雌激素受体有明显的相互作用。这种相互作用是弱雌激素的特征，具有潜在的抗雌激素活性（孵育时间和温度增加时RBA值降低）。结果与体内获得的数据高度一致。此外，这些化合物中的一些也在一定程度上与雄激素受体相互作用。将讨论结果以概述这些系列中的一些构效关系。
