Antiproliferative and Antimetastatic Properties of 16-Azidomethyl Substituted 3-O-Benzyl Estrone Analogs

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.

LINC00173 silence and estrone supply suppress ER+ breast cancer by estrogen receptor α degradation and LITAF activation

“…Notably, this finding aligns with recent reports indicating that the E1 analogues 16AABE and 16BABE can inhibit the proliferation and metastasis of BC cells. 22 Overall, our findings highlight the different effects of estrogen types on the development and potential treatment of ER + BC. These results provide crucial preclinical research data for precision drug selection among relevant populations.…”

“…The appropriate combination of silencing LINC00173 and E1 demonstrates effective inhibition of ER + BC. 22 …”