抗雌激素活性化合物及其构效关系研究

Studies on antiestrogen compounds and their structure-activity relationships

抗雌激素疗法是雌激素受体依赖性乳腺癌内分泌疗法的重要手段之一。抗雌激素化合物按作用机制分类可分为选择性雌激素受体调节剂和纯抗雌激素剂,其结构类型主要包括取代雌二醇衍生物、三苯乙烯、苯骈杂环类及多酚类天然化合物。本文重点综述近年来抗雌激素化合物的作用机制、构效关系及其研究进展。

Antiestrogens have been proven to be highly effective in the treatment of estrogen receptor-dependent breast cancer.According to the mechanism,antiestrogen compounds were mainly categorized as selective estrogen receptor modulators（SERM）and pure antiestrogens,which structurally include estradiol derivatives,triphenylethylenes,benzo heterocyclic and polyphenol of natural compounds.The research advances on the antiestrogen compounds and their structure-activity relationships are reviewed.