【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.更多还原

【Abstract】 Based on the anticancer activity and structural characters of β-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.更多还原