Synthesis and biological evaluation of 13α-estrone derivatives as potential antiproliferative agents

Szabó, Johanna and Pataki, Zoltán and Wölfling, János and Schneider, Gyula and Bózsity, Noémi and Minorics, Renáta and Zupkó, István and Mernyák, Erzsébet (2016) Synthesis and biological evaluation of 13α-estrone derivatives as potential antiproliferative agents. STEROIDS, 113. pp. 14-21. ISSN 0039-128X

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Abstract

13 alpha-Estrone derivatives containing various substituents on C-3 and C-17 were synthesized, and evaluated by means of MU assays for in vitro antiproliferative activity against a panel of human adherent cancer cell lines (HeLa, MCF-7, A2780 and A431). Compounds with N-benzyltriazolylmethoxy moieties on C-3 proved to be more potent than their 3-hydroxy or 3-ether counterparts. Some triazoles exerted substantial cytostatic effects against particular tumor cell lines, with submicromolar IC50 values.

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