摘要
目的:对槐定碱进行结构改造,合成新型槐定碱衍生物,研究其抗肿瘤活性。方法:以槐定碱为原料,合成了8个14位取代槐定碱衍生物,其结构经1H-NMR,MS证实。经MTT法筛选了衍生物对肝癌、肺癌、结肠癌、胃癌、神经胶质瘤、脑胶质瘤、宫颈癌以及黑色素瘤的抗癌活性。结果:合成的8个槐定碱衍生物中有6个是14位不同构型的槐定碱衍生物。实验显示14位为氯取代的化合物①、②、③和⑧对大部分肿瘤细胞的抑制活性均明显高于槐定碱。结论:在槐定碱14位引入氯原子取代可提高槐定碱的抗肿瘤活性。
Objective ：To study the relationship between the novel sophoridine derivatives which synthesized by structural modification and its antitumor activity. Method ：8 sophoridine derivatives which substituted at 14 position have been synthesized and their structures were conformed by 1 H - NMR and MS. The antitumor activities against such as live cancer, lung cancer, colon cancer, gastric cancer, glioblastomas, cervical cancer, melanoma were determined by MTT methods. Results：6 out of total 8 compounds were sophoridine derivatives with different configuration at 14 position. Results showed the antitumor activites of 14 - chloro substitued compounds 1,2, 3, 8 are better than sophoridine in most tumor cells. Conclusion：Substitution by chlorine at 14 position of sophoridine can enhance the antitumor activity of sophoridine.
出处
《天津药学》
2013年第4期1-5,共5页
Tianjin Pharmacy
关键词
槐定碱
抗肿瘤
结构改造
合成
sophoridine
antitumor
structural modification
synthesis
