机构地区: 广西师范大学化学化工学院省部共建药用资源化学与药物分子工程教育部重点实验室
出 处: 《广西师范大学学报(自然科学版)》 2012年第2期78-82,共5页
摘 要: 以DNA双螺旋结构为靶点,设计合成了一系列新的6-取代的氧化异阿朴菲生物碱衍生物3a~3e。所有化合物的结构均用ESI-MS,1HNMR和元素分析确认。运用紫外吸收光谱研究了氧化异阿朴菲生物碱衍生物与小牛胸腺DNA(ctDNA)的相互作用。用MTT法评价衍生物对HepG2、SGC-7901、SW480、786-O和NCI-H460 5种肿瘤细胞的毒性。光谱研究结果表明衍生物能与ctDNA发生嵌插结合作用,细胞毒性测试表明衍生物具有中等强度的抗肿瘤活性。 A series of novel 6-Substituted 1-Azabenzanthrone derivatives 3a-3e had been synthesized based on double helix DNA. All the target compounds were characterized by ESI-MS,1H NMR and element analysis. The interaction of derivatives with calf thymus DNA was performed by UV spectra. The in vitro cytotoxicity of derivatives for five cell lines (HepG2,SGC-7901,SW480,786-0 and NCI-H460) was evaluated using MTT method. The experimental results indicated that the derivatives could intercalate calf thymus DNA and showed moderate cytotoxicity against different tumor cell lines.