Synthesis of novel steroidal 17α-triazolyl derivatives via Cu(I)-catalyzed azide-alkyne cycloaddition, and an evaluation of their cytotoxic activity in vitro

Éva Frank, Judit Molnár, István Zupkó, Zalán Kádár, János Wölfling

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Abstract

Regioselective Cu(I)-catalyzed 1,3-dipolar cycloaddition of steroidal 17α-azides with different terminal alkynes afforded novel 1,4-disubstituted triazolyl derivatives in good yields in both the estrone and the androstane series. The antiproliferative activities of the structurally related triazoles were determined in vitro on three malignant human cell lines (HeLa, MCF7 and A431), with the microculture tetrazolium assay.

Original languageEnglish
Pages (from-to)1141-1148
Number of pages8
JournalSteroids
Volume76
Issue number10-11
DOIs
Publication statusPublished - Sep 1 2011

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Keywords

  • Cycloaddition
  • Cytotoxic activity
  • Regioselectivity
  • Triazoles

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Endocrinology
  • Pharmacology
  • Clinical Biochemistry
  • Organic Chemistry

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