非甾体雌激素和抗雌激素：芪及芪二醇环丙基类似物的生物活性

Nonsteroidal estrogens and antiestrogens: biological activity of cyclopropyl analogs of stilbene and stilbenediol.

作者信息

Pento J T, Magarian R A, Wright R J, King M M, Benjamin E J

出版信息

J Pharm Sci. 1981 Apr;70(4):399-403. doi: 10.1002/jps.2600700415.

Abstract

The estrogenic, antiestrogenic, and receptor binding activity of a series of cyclopropyl analogs of stilbene and stilbenediol were determined using the uterotropic assay in the mouse and the receptor binding assay with rat uterine cytosol. One compound, 1,1-dichloro-cis-2,3-diphenylcyclopropane (II), displayed antiestrogenic activity in vivo with a low affinity for the estrogen receptor in vitro and showed tumor remission activity on 7,12-dimethylbenz(a)anthracene-induced estrogen-dependent rat mammary tumors. Compounds VIII, IV, and V (in that order) exhibited the greatest estrogen activity in the mouse and the greatest receptor binding activity in vitro. Compound VIII exhibited antifertility activity in the mouse.

摘要

使用小鼠子宫增重试验和大鼠子宫胞质溶胶受体结合试验，测定了一系列芪和芪二醇环丙基类似物的雌激素活性、抗雌激素活性及受体结合活性。一种化合物，即1,1 - 二氯 - 顺式 - 2,3 - 二苯基环丙烷（II），在体内表现出抗雌激素活性，在体外对雌激素受体的亲和力较低，并且对7,12 - 二甲基苯并(a)蒽诱导的雌激素依赖性大鼠乳腺肿瘤具有肿瘤缓解活性。化合物VIII、IV和V（按此顺序）在小鼠中表现出最大的雌激素活性，在体外表现出最大的受体结合活性。化合物VIII在小鼠中表现出抗生育活性。