【摘要】 目的:以甜菊苷为原料合成ent-贝壳杉烯类目标化合物。方法:构造了以exo-亚甲基环戊酮为特征的药效基团结构,同时对C-4位的羧基进行了修饰,以改善目标化合物的活性,并通过MTT法检测目标化合物的体外抗肿瘤活性。结果和结论:合成的13个ent-贝壳杉烯类目标化合物结构经1HNMR、ESI-MS和FT-IR确认。MTT法显示部分目标化合物对肿瘤细胞BEL-7402,HO-8910,MCF-7和HL-60有较好的抑制活性。更多还原

【Abstract】 Aim:To synthesize the ent-kaurene diterpenoid and its derivatives from natural available stevioside.Methods:The crucial pharmacophore of exo-methylene ketone was designed and the carboxyl group at C-4 was modified.The cytotoxic inhibition activities in vitro of target compounds were evaluated against human cancer cells BEL-7402,HO-8910,MCF-7 and HL-60 by a MTT method.Results and Conclusion:The structures of new target compounds were identified by 1H NMR,FT-IR and EI-MS.The preliminary experimental results showed that some derivatives of ent-kaurene diterpenoid possessed fair inhibitory activity against tumor cell lines compared with that of their parent steviol.更多还原