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

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 outstan...

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Bibliographic Details
Main Authors: Senobar Tahaei Seyyed Ashkan
Kulmány Ágnes
Minorics Renáta
Kiss Anita
Szabó Zoltán
Germán Péter
Szebeni Gábor
Gémes Nikolett
Mernyák Erzsébet
Zupkó István
Format: Article
Published: 2023
Series:INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES 24 No. 18
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doi:10.3390/ijms241813749

mtmt:34131836
Online Access:http://publicatio.bibl.u-szeged.hu/28365
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Summary: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.
Physical Description:16
ISSN:1661-6596