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Molecules 2018, 23(9), 2243;

Design and Synthesis of Novel Dehydroepiandrosterone Analogues as Potent Antiproliferative Agents

Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002, China
Authors to whom correspondence should be addressed.
Received: 16 August 2018 / Revised: 30 August 2018 / Accepted: 31 August 2018 / Published: 3 September 2018
(This article belongs to the Section Organic Chemistry)
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The aim of the present study was to determine the cytotoxic effects of a series of novel dehydroepiandrosterone derivatives containing triazole at the C16 position on human cancer cells. The cancer cells used in the present study were A549, Hela, HepG-2, BEL7402, MCF-7, and HCT116. Several of the synthesised compounds exhibited potent antiproliferative effects. The most promising compound was (E)-3-hydroxy-16-((1-(4-iodophenyl)-1H-1,2,3-triazole-4-yl)methylene)-10,13-dimet-hyl-1,3,4,7,8,9,10,11,12,13,15,16-dodecahydro-2H-cyclopenta[a]phenanthren-17(14)-one (compound 2n), which showed considerably high antiproliferative activity in the HepG-2 cell line, with an IC50 value of 9.10 µM, and considerably high activity against the MCF-7 cell line, with an IC50 value of 9.18 µM. Flow cytometry assays demonstrated that compound 2n exerted antiproliferative effects by arresting cells in the G2 phase of the cell cycle and inducing apoptosis. View Full-Text
Keywords: dehydroepiandrosterone; 1,2,3-Triazoles; antiproliferative; synthesis dehydroepiandrosterone; 1,2,3-Triazoles; antiproliferative; synthesis

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Huang, X.; Shen, Q.-K.; Zhang, H.-J.; Li, J.-L.; Tian, Y.-S.; Quan, Z.-S. Design and Synthesis of Novel Dehydroepiandrosterone Analogues as Potent Antiproliferative Agents. Molecules 2018, 23, 2243.

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