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