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Novel Hybrid Molecules on the Basis of Steroids and (5Z,9Z)-Tetradeca-5,9-dienoic Acid: Synthesis, Anti-Cancer Studies and Human Topoisomerase I Inhibitory Activity

[ Vol. 17 , Issue. 8 ]


  Pages 1126 - 1135 ( 10 )


Novel steroid derivatives of 5Z,9Z-dienoic acids were prepared by the DCC/DMAP-catalyzed esterification of (5Z,9Z)-tetradeca-5,9-dienoic acid with hydroxy steroids. High cytotoxicity towards the HEK293, Jurkat, K562 cancer cell lines and human topoisomerase I (hTop1) inhibitory activity in vitro were found for the synthesized acids. A probable mechanism of topoisomerase I inhibition was hypothesized on the basis of in silico studies resorting to docking.


5Z, 9Z-Dienoic acids, steroids, cross-cyclomagnesiation, homogeneous catalysis, 1, 2-dienes, topoisomerase I inhibitors, cancer cell lines, docking.

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