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© 2023 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.

Abstract

Four diastereomers of 16-azidomethyl substituted 3-O-benzyl estradiol (14) 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.

Details

Title
Antiproliferative and Antimetastatic Properties of 16-Azidomethyl Substituted 3-O-Benzyl Estrone Analogs
Author
Seyyed Ashkan Senobar Tahaei 1 ; Kulmány, Ágnes 1 ; Minorics, Renáta 1 ; Kiss, Anita 2   VIAFID ORCID Logo  ; Szabó, Zoltán 3   VIAFID ORCID Logo  ; Péter Germán 1 ; Szebeni, Gábor J 4   VIAFID ORCID Logo  ; Gémes, Nikolett 4 ; Mernyák, Erzsébet 2 ; Zupkó, István 5   VIAFID ORCID Logo 

 Institute of Pharmacodynamics and Biopharmacy, University of Szeged, H-6720 Szeged, Hungary 
 Department of Inorganic, Organic and Analytical Chemistry, University of Szeged, H-6720 Szeged, Hungary 
 Department of Medicinal Chemistry, University of Szeged, H-6720 Szeged, Hungary 
 Laboratory of Functional Genomics, Biological Research Centre, H-6726 Szeged, Hungary 
 Institute of Pharmacodynamics and Biopharmacy, University of Szeged, H-6720 Szeged, Hungary; Interdisciplinary Centre of Natural Products, University of Szeged, H-6720 Szeged, Hungary 
First page
13749
Publication year
2023
Publication date
2023
Publisher
MDPI AG
ISSN
16616596
e-ISSN
14220067
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2869382249
Copyright
© 2023 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.