新型24-氨基-25,26,27-三降羊毛甾-8-烯的合成：U937细胞中的细胞毒性和凋亡潜力
Synthesis of novel 24-amino-25,26,27-trinorlanost-8-enes: cytotoxic and apoptotic potential in U937 cells.
作者信息
O'Keeffe Roisin, Kenny Olivia, Brunton Nigel P, Hossain Mohammad B, Rai Dilip K, Jones Peter W, O'Brien Nora, Maguire Anita R, Collins Stuart G
机构信息
Department of Chemistry, Analytical and Biological Chemistry Research Facility, Synthesis and Solid State Pharmaceutical Centre, University College Cork, Ireland.
School of Food and Nutritional Sciences, University College Cork, Ireland.
出版信息
Bioorg Med Chem. 2015 May 1;23(9):2270-80. doi: 10.1016/j.bmc.2015.02.034. Epub 2015 Mar 5.
In the present study, the synthesis of a range of novel 24-amino-25,26,27-trinorlanost-8-ene derivatives including 24-piperadino-trinorlanost-8-enes, 24-piperazino-trinorlanost-8-enes, 24-morpholino-trinorlanost-8-enes, and 24-diethylamino-trinorlanost-8-enes is reported and their cytotoxic and apoptotic potential evaluated in U937 cell lines. Excellent IC₅₀ results for piperidine and 1-(2-hydroxyethyl)piperazine derivatives have been observed (IC₅₀ values of 1.9 μM and 2.7 μM in U937 cells, respectively).
在本研究中，报告了一系列新型24-氨基-25,26,27-三降羊毛甾-8-烯衍生物的合成，包括24-哌啶基-三降羊毛甾-8-烯、24-哌嗪基-三降羊毛甾-8-烯、24-吗啉基-三降羊毛甾-8-烯和24-二乙氨基-三降羊毛甾-8-烯，并在U937细胞系中评估了它们的细胞毒性和凋亡潜力。已观察到哌啶和1-(2-羟乙基)哌嗪衍生物具有出色的IC₅₀结果（在U937细胞中的IC₅₀值分别为1.9 μM和2.7 μM）。
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