ent-贝壳杉烯类化合物的合成及其抗肿瘤活性  

Synthesis and antitumor activity of ent-kaurene diterpenoids

作　　者：张大永[1] 汤湧 王可[1] 吴晓明[1] 华维一[1] 

机构地区：[1]中国药科大学新药研究中心,南京210009

出　　处：《中国药科大学学报》2010年第1期20-25,共6页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.30973607);江苏省“六大人才高峰”资助项目(No.Y092003)~~

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。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.

关 键 词：ent-贝壳杉烯 甜菊苷 exo-亚甲基环戊酮 抗肿瘤活性 合成 

分 类 号：R914[医药卫生—药物化学] R96[医药卫生—药学]