PDF(Pubmed)
Abstract：
Four diastereomers of 16-azidomethyl substituted 3-O-benzyl estradiol (1-4) and their two estrone analogs (16AABE and 16BABE) were tested for their antiproliferative properties against human gynecological cancer cell lines. The estrones were selected for additional experiments based on their outstanding cell growth-inhibiting activities. Both compounds increased hypodiploid populations of breast cancer cells, and 16AABE elicited cell cycle disturbance as evidenced by flow cytometry. The two analogs substantially increased the rate of tubulin polymerization in vitro. 16AABE and 16BABE inhibited breast cancer cells\' migration and invasive ability, as evidenced by wound healing and Boyden chamber assays. Since both estrone analogs exerted remarkable estrogenic activities, as documented by a luciferase reporter gene assay, they can be considered as promising drug candidates for hormone-independent malignancies.
摘要：
测试了16-叠氮基甲基取代的3-O-苄基雌二醇（1-4）的四种非对映异构体及其两种雌酮类似物（16AABE和16BABE）对人妇科癌细胞系的抗增殖特性。根据其出色的细胞生长抑制活性，选择雌酮用于其他实验。两种化合物都增加了乳腺癌细胞的亚二倍体群体，和16AABE引起细胞周期紊乱，如流式细胞术所证明的。这两种类似物在体外显著增加了微管蛋白聚合的速率。16AABE和16BABE抑制乳腺癌细胞的迁移和侵袭能力，伤口愈合和Boyden室试验证明了这一点。由于两种雌酮类似物都具有显着的雌激素活性，正如荧光素酶报告基因测定法所记录的那样，它们可以被认为是治疗激素非依赖性恶性肿瘤的有希望的候选药物.
