6-取代1-氮杂苯并蒽酮衍生物的合成及抗肿瘤活性研究

Synthesis and Antitumor Activity of 6-Substituted 1-Azabenzanthrone

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.