摘要
目的:设计合成β-榄香烯单取代胺类衍生物,并探讨该类衍生物的体外抗肿瘤活性。方法:通过亲核取代反应合成β-榄香烯单取代胺类衍生物,采用WST-1法对它们的体外抗肿瘤活性进行评价。结果:合成得到了8个目标化合物(均未见文献报道),并利用1H NMR,MS,IR对其结构进行了表征。细胞试验表明:β-榄香烯单取代胺类衍生物对人白血病细胞(K562细胞)及人宫颈癌细胞(HeLa细胞)的体外抗增殖活性与β-榄香烯相比有了明显提高。结论:β-榄香烯单取代胺衍生物的抗肿瘤活性较β-榄香烯明显提高。
Aim：To design and synthesize a series of β-elemene amine derivatives in order to investigate their in vitro antitumor activity. Methods： The target compounds were synthesized via nucleophilic substitution. Their antitumor activity in vitro were evaluated by WST-1 method. Results： Eight new target compounds were synthesized. Their structures were characterized by IR, 1H NMR and MS. Their in vitro antitumor activity in K562 cell and HeLa cell lines were improved compared to that of β-elemene. amine derivatives were improved significantly.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2007年第5期396-399,共4页
Journal of China Pharmaceutical University
基金
基金项目中国科学院百人计划资助项目(No.26200601)~~
关键词
β-榄香烯衍生物
单取代胺
合成
抗肿瘤活性
β-elemene derivatives
monosubstituted amine
synthesis
antitumor activity of β-elemene monosubstituted
