Literature DB >> 27928953

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.

Vladimir A D'yakonov1, Lilya U Dzhemileva2, Regina A Tuktarova1, Svetlana R Ishmukhametova1, Milyausha M Yunusbaeva3, Ilfir R Ramazanova1, Usein M Dzhemilev1.   

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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

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Keywords:  1; 2-dienes; 5Z; 9Z-Dienoic acids; cancerzzm321990cell lines; cross-cyclomagnesiation; docking; homogeneous catalysis; steroids; topoisomerase I inhibitors

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Year:  2017        PMID： 27928953     DOI： 10.2174/1871520616666161207154850

Source DB:  PubMed          Journal:  Anticancer Agents Med Chem        ISSN： 1871-5206            Impact factor:   2.505


  2 in total

1.  Limonoids Containing a C₁⁻O⁻C29 Moiety: Isolation, Structural Modification, and Antiviral Activity.

Authors:  Jing-Ling Ren; Xiao-Peng Zou; Wan-Shan Li; Li Shen; Jun Wu
Journal:  Mar Drugs       Date:  2018-11-04       Impact factor: 5.118

2.  Synthesis and Anticancer Activity of Hybrid Molecules Based on Lithocholic and (5Z,9Z)-Tetradeca-5,9-dienedioic Acids Linked via Mono(di,tri,tetra)ethylene Glycol and α,ω-Diaminoalkane Units.

Authors:  Vladimir A D'yakonov; Regina A Tuktarova; Lilya U Dzhemileva; Svetlana R Ishmukhametova; Usein M Dzhemilev
Journal:  Pharmaceuticals (Basel)       Date:  2021-01-23
  2 in total

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