β-卡波林生物碱flazin与冬凌草甲素杂合衍生物的合成及其抗肿瘤活性  

Synthesis of hybrid derivatives ofβ-carboline flazin and oridonin with anticancer activity

作　　者：李莉 路明坤 连国 周义博 孙焕 刘吉开[1] LI Li;LU Mingkun;LIAN Guo;ZHOU Yibo;SUN Huan;LIU Jikai(School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan 430074, China)

机构地区：[1]中南民族大学药学院,武汉430074

出　　处：《中南民族大学学报（自然科学版）》2021年第6期568-573,共6页Journal of South-Central University for Nationalities：Natural Science Edition

基　　金：国家自然科学基金资助项目(81803395);湖北省自然科学基金资助项目(2018CFB222);中南民族大学大学生创新训练计划项目(GCX2027)。

摘　　要：基于β-卡波林生物碱flazin和冬凌草甲素的抗肿瘤活性及分子结构特点,对其进行结构修饰,合成了一系列类似物,并利用活性官能团拼接原理,将二者进行杂合获得杂合衍生物.采用改良MTT法研究了杂合衍生物对肿瘤细胞增殖的影响,初步确定了具有良好细胞毒性的活性分子,为获得更为低毒、高效的抗肿瘤先导化合物提供了线索.Based on the anticancer activity and structural characters ofβ-carboline flazin and oridonin,a series of flazin and oridonin analogues were synthesized by structural modification.Hybridized derivatives were then obtained by combining flazin and oridonin by the means of grafting.The influence of hybridized derivatives on tumor cell proliferation were investigated using improved MTT evaluation,which were preliminarily identified as active compounds with good cytotoxicity and provided clues for further development of anti-cancer leading compounds with low toxicity and high efficiency.

关 键 词：β-卡波林 冬凌草甲素 杂合化合物 抗肿瘤活性 

分 类 号：O621.3[理学—有机化学]