Literature DB >> 27263437

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

Johanna Szabó1, Zoltán Pataki1, János Wölfling1, Gyula Schneider1, Noémi Bózsity2, Renáta Minorics2, István Zupkó3, Erzsébet Mernyák4.   

Abstract

13α-Estrone derivatives containing various substituents on C-3 and C-17 were synthesized, and evaluated by means of MTT 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.
Copyright © 2016 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  13α-Estrone; 17-Deoxy-13α-estrone; Antiproliferative effect; Azide-alkyne cycloaddition

Mesh：

Substances：

Year:  2016        PMID： 27263437     DOI： 10.1016/j.steroids.2016.05.010

Source DB:  PubMed          Journal:  Steroids        ISSN： 0039-128X            Impact factor:   2.668


  7 in total

1.  Synthesis of novel 13α-estrone derivatives by Sonogashira coupling as potential 17β-HSD1 inhibitors.

Authors:  Ildikó Bacsa; Rebeka Jójárt; János Wölfling; Gyula Schneider; Bianka Edina Herman; Mihály Szécsi; Erzsébet Mernyák
Journal:  Beilstein J Org Chem       Date:  2017-06-30       Impact factor: 2.883

2.  The first Pd-catalyzed Buchwald-Hartwig aminations at C-2 or C-4 in the estrone series.

Authors:  Ildikó Bacsa; Dávid Szemerédi; János Wölfling; Gyula Schneider; Lilla Fekete; Erzsébet Mernyák
Journal:  Beilstein J Org Chem       Date:  2018-05-04       Impact factor: 2.883

3.  In Vitro and In Vivo Anti-Breast Cancer Activities of Some Synthesized Pyrazolinyl-estran-17-one Candidates.

Authors:  Abd El-Galil E Amr; Mohamed El-Naggar; Mohamed A Al-Omar; Elsayed Ahmed Elsayed; Mohamed M Abdalla
Journal:  Molecules       Date:  2018-06-28       Impact factor: 4.411

4.  Transition metal-catalysed A-ring C-H activations and C(sp2)-C(sp2) couplings in the 13α-oestrone series and in vitro evaluation of antiproliferative properties.

Authors:  Péter Traj; Ali Hazhmat Abdolkhaliq; Anett Németh; Sámuel Trisztán Dajcs; Ferenc Tömösi; Tea Lanisnik-Rizner; István Zupkó; Erzsébet Mernyák
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

5.  Synthesis and Biological Evaluation of Triazolyl 13α-Estrone-Nucleoside Bioconjugates.

Authors:  Brigitta Bodnár; Erzsébet Mernyák; János Wölfling; Gyula Schneider; Bianka Edina Herman; Mihály Szécsi; Izabella Sinka; István Zupkó; Zoltán Kupihár; Lajos Kovács
Journal:  Molecules       Date:  2016-09-10       Impact factor: 4.411

6.  Synthesis of Novel C-2- or C-15-Labeled BODIPY-Estrone Conjugates.

Authors:  Ildikó Bacsa; Csilla Konc; Anna Boglárka Orosz; Gábor Kecskeméti; Réka Rigó; Csilla Özvegy-Laczka; Erzsébet Mernyák
Journal:  Molecules       Date:  2018-04-03       Impact factor: 4.411

7.  Synthesis and evaluation of anticancer activities of 2- or 4-substituted 3-(N-benzyltriazolylmethyl)-13α-oestrone derivatives.

Authors:  Rebeka Jójárt; Seyyed Ashkan Senobar Tahaei; Péter Trungel-Nagy; Zoltán Kele; Renáta Minorics; Gábor Paragi; István Zupkó; Erzsébet Mernyák
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051
  7 in total

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