[3,3'-二羟基-α,β-二乙基芪型新型抗雌激素的研制及其对二甲基苯并蒽诱导的SD大鼠激素依赖性乳腺癌的评价（作者译）]
[Development of new antiestrogens of the 3,3'-dihydroxy-alpha, beta-diethylstilbene-type and their evaluation on the DMBA-induced hormone dependent mammary carcinoma of the SD-rat (author's transl)].
作者信息
Kranzfelder G, Schneider M, von Angerer E, Schönenberger H
出版信息
J Cancer Res Clin Oncol. 1980;97(2):167-86. doi: 10.1007/BF00409903.
Abstract
The displacement of the phenolic OH-group of diethylstilbestrol into the 3,3'-position (trans-3,3'-dihydroxy-alpha, beta-diethylstilbene, compd. III) leads to a strong decrease of the estrogenic effect under conservation of the receptor affinity. In vitro, III inhibits the estradiol-receptor-interaction competitively and, in vivo, antagonises the uterotropic effect of estrone in the mouse. In tests with the DMBA-induces, hormone-dependent mammary carcinoma of the rat a dose-dependent strong decrease of tumor size and yield is achieved under the influence of III, due to the antiestrogenic properties of III. The replacement of the alpha, beta-bound ethyl groups in III by other alkyl chains leads to no further increase of the antiestrogenic and antitumor activity.
摘要
己烯雌酚的酚羟基位移至3,3'-位（反式-3,3'-二羟基-α,β-二乙芪，化合物III）会导致雌激素效应大幅降低，而受体亲和力得以保留。在体外，III竞争性抑制雌二醇与受体的相互作用，在体内，III拮抗雌酮对小鼠子宫的促生长作用。在对二甲基苯并蒽诱导的大鼠激素依赖性乳腺癌进行的试验中，由于III的抗雌激素特性，在其影响下肿瘤大小和产量呈剂量依赖性大幅降低。将III中α,β位连接的乙基替换为其他烷基链不会进一步增强其抗雌激素和抗肿瘤活性。
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