Journal
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
Volume 17, Issue 8, Pages 1126-1135Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1871520616666161207154850
Keywords
5Z,9Z-Dienoic acids; steroids; cross-cyclomagnesiation; homogeneous catalysis; 1,2-dienes; topoisomerase I inhibitors; cancer cell lines; docking
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Funding
- Russian Science Foundation [14-13-00263]
- Russian Science Foundation [14-13-00263] Funding Source: Russian Science Foundation
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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.
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