Molecules 2011, 16(6), 4786-4806; doi:10.3390/molecules16064786
Article

Synthesis and In Vitro Antiproliferative Activity of Novel Androst-5-ene Triazolyl and Tetrazolyl Derivatives

1,* email, 1, 1, 1, 2, 2, 3,4 and 1,* email
Received: 12 May 2011; in revised form: 2 June 2011 / Accepted: 6 June 2011 / Published: 9 June 2011
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: A straightforward and reliable method for the regioselective synthesis of steroidal 1,4-disubstituted triazoles and 1,5-disubstituted tetrazoles via copper(I)-catalyzed cycloadditions is reported. Heterocycle moieties were efficiently introduced onto the starting azide compound 3β-acetoxy-16β-azidomethylandrost-5-en-17β-ol through use of the “click” chemistry approach. The antiproliferative activities of the newly-synthesized triazoles were determined in vitro on three human gynecological cell lines (HeLa, MCF7 and A2780) using the microculture tetrazolium assay.
Keywords: click chemistry; steroid azides; triazoles; tetrazoles; CuAAC
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MDPI and ACS Style

Kádár, Z.; Kovács, D.; Frank, É.; Schneider, G.; Huber, J.; Zupkó, I.; Bartók, T.; Wölfling, J. Synthesis and In Vitro Antiproliferative Activity of Novel Androst-5-ene Triazolyl and Tetrazolyl Derivatives. Molecules 2011, 16, 4786-4806.

AMA Style

Kádár Z, Kovács D, Frank É, Schneider G, Huber J, Zupkó I, Bartók T, Wölfling J. Synthesis and In Vitro Antiproliferative Activity of Novel Androst-5-ene Triazolyl and Tetrazolyl Derivatives. Molecules. 2011; 16(6):4786-4806.

Chicago/Turabian Style

Kádár, Zalán; Kovács, Dóra; Frank, Éva; Schneider, Gyula; Huber, Judit; Zupkó, István; Bartók, Tibor; Wölfling, János. 2011. "Synthesis and In Vitro Antiproliferative Activity of Novel Androst-5-ene Triazolyl and Tetrazolyl Derivatives." Molecules 16, no. 6: 4786-4806.

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