[(三乙基硅基)乙炔基]雌二醇类似物作为潜在的抗生育剂。

Analogues of [(triethylsilyl)ethynyl]estradiol as potential antifertility agents.

作者信息

Peters R H, Crowe D F, Avery M A, Chong W K, Tanabe M

机构信息

Bio-Organic Chemistry Laboratory, SRI International, Menlo Park, California 94025.

出版信息

J Med Chem. 1988 Mar;31(3):572-6. doi: 10.1021/jm00398a014.

DOI:10.1021/jm00398a014

PMID:3346872

Abstract

Various 17 alpha-ethynylsteroids were prepared and derivatized as the corresponding triethylsilyl compounds 2-35, which were examined for a ratio of antifertility to estrogenic activity that would be more beneficial than that of the presently used agent. Among the triethylsilyl compounds evaluated, only 23 displayed this desired ratio, although two other compounds without the triethylsilyl moiety, 18 and 26, shared similar characteristics.

摘要

制备了多种17α-乙炔基甾体，并将其衍生化为相应的三乙基硅基化合物2 - 35，对这些化合物的抗生育活性与雌激素活性之比进行了检测，以期得到比目前使用的药物更有益的比例。在所评估的三乙基硅基化合物中，只有23表现出这种理想的比例，尽管另外两种没有三乙基硅基部分的化合物18和26也具有相似的特性。