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

作者：D'yakonov Vladimir A^*; Dzhemileva Lilya U^*; Tuktarova Regina A; Ishmukhametova Svetlana R; Yunu**aeva Milyausha M; Ramazanov Ilfir R; Dzhemilev Usein M

来源：Anti-Cancer Agents in Medicinal Chemistry, 2017, 17(8): 1126-1135.

DOI：10.2174/1871520616666161207154850

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

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.

• 出版日期2017