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.
