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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 ]

Author(s):

Vladimir A. D'yakonov, Lilya U. Dzhemileva, Regina A. Tuktarova, Svetlana R. Ishmukhametova, Milyausha M. Yunusbaeva, Ilfir R. Ramazanova and Usein M. Dzhemilev   Pages 1126 - 1135 ( 10 )

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.

Affiliation:

Institute of Petrochemistry and Catalysis, Russian Academy of Science, 141 Prospekt Oktyabrya, 450075, Ufa, Department of Immunology and Human Reproductive Health, Bashkir State Medical University, 3 Lenin Street, 450003, Ufa, Institute of Petrochemistry and Catalysis, Russian Academy of Science, 141 Prospekt Oktyabrya, 450075, Ufa, Institute of Petrochemistry and Catalysis, Russian Academy of Science, 141 Prospekt Oktyabrya, 450075, Ufa, Institute of Biochemistry and Genetics, Ufa Research Center, Russian Academy of Sciences 71 Prospect Oktyabrya, 450054, Ufa, Institute of Petrochemistry and Catalysis, Russian Academy of Science, 141 Prospekt Oktyabrya, 450075, Ufa, Institute of Petrochemistry and Catalysis, Russian Academy of Science, 141 Prospekt Oktyabrya, 450075, Ufa

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