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Anti-Cancer Agents in Medicinal Chemistry

Author(s): Vladimir A. D’yakonov*, Lilya U. Dzhemileva*, Regina A. Tuktarova, Svetlana R. Ishmukhametova, Milyausha M. Yunusbaeva, Ilfir R. Ramazanov and Usein M. Dzhemilev

DOI: 10.2174/1871520616666161207154850

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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

Page: [1126 - 1135] Pages: 10

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Abstract

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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