设计和合成新型去氢表雄酮类似物作为有效的抗增殖剂。
Design and Synthesis of Novel Dehydroepiandrosterone Analogues as Potent Antiproliferative Agents.
机构信息
Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002, China.
出版信息
Molecules. 2018 Sep 3;23(9):2243. doi: 10.3390/molecules23092243.
The aim of the present study was to determine the cytotoxic effects of a series of novel dehydroepiandrosterone derivatives containing triazole at the C 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 ()-3-hydroxy-16-((1-(4-iodophenyl)-1-1,2,3-triazole-4-yl)methylene)-10,13-dimet-hyl-1,3,4,7,8,9,10,11,12,13,15,16-dodecahydro-2-cyclopenta[a]phenanthren-17(14)-one (compound ), which showed considerably high antiproliferative activity in the HepG-2 cell line, with an IC value of 9.10 µM, and considerably high activity against the MCF-7 cell line, with an IC value of 9.18 µM. Flow cytometry assays demonstrated that compound exerted antiproliferative effects by arresting cells in the G2 phase of the cell cycle and inducing apoptosis.
本研究旨在确定一系列新型含三唑的 C 位去氢表雄酮衍生物对人癌细胞的细胞毒性作用。本研究中使用的癌细胞为 A549、Hela、HepG-2、BEL7402、MCF-7 和 HCT116。几种合成的化合物表现出很强的抗增殖作用。最有前途的化合物是()-3-羟基-16-((1-(4-碘苯基)-1-1,2,3-三唑-4-基)亚甲基)-10,13-二甲基-1,3,4,7,8,9,10,11,12,13,15,16-十二氢-2-环戊[a]菲并[17(14)]-17(14)-酮（化合物），它在 HepG-2 细胞系中表现出相当高的抗增殖活性，IC 值为 9.10 µM，对 MCF-7 细胞系的活性也相当高，IC 值为 9.18 µM。流式细胞术检测表明，化合物通过将细胞周期 G2 期阻滞并诱导细胞凋亡发挥抗增殖作用。
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