3-取代吲哚酮类化合物的合成及抗肿瘤活性  

Synthesis and the antitumor activities of 3-substituted indolin-2-ones

作　　者：闵真立[1] 姜凤超[1] 张奇[1] 

机构地区：[1]华中科技大学同济医学院药学院,湖北武汉430030

出　　处：《中国药物化学杂志》2005年第3期129-132,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计合成具有抗肿瘤活性的3-取代吲哚-2-酮类化合物,并对其抗肿瘤活性进行评价。方法以吲哚酮和苯甲醛衍生物在微波辐射条件下进行缩合反应制得目标化合物,用人肝癌HepG2细胞进行抗肿瘤活性检测。结果合成了8个化合物,其中6个未见报道。其结构均经1HNMR、IR及ESIMS确证。结论初步抗肿瘤活性测试结果显示化合物Ⅱe、Ⅱg有较强的活性(IC50值分别为1.4μmol·L-1和1.2μmol·L-1,小于阳性对照药5Fu)。微波辐射技术用于3取代吲哚酮的合成,能大幅度缩短反应时间,提高收率。Aim To design and synthesize 3-substituted indolin-2-ones and to determine their antitumor activities in vitro.Method Eight compounds were synthesized by condensation between oxindole and benzaldehyde derivatives under microwave irradiation,and their antitumor activities were assayed using human HepG_2 cells.Result Six compounds were so far unreported and all the eight target compounds were identified by 1H-NMR,IR,ESI-MS.Conclusion Preliminary bioassay suggests that compound Ⅱe(IC_ 50 1.4 μmol·L -1)and Ⅱg(1.2 μmol·L -1)display good antitumor activities.Synthesis of 3-substitued indolin-2-ones under microwave irradiation can shorten reaction time and result in better yields.

关 键 词：药物化学 化合物制备 微波辐射 3-取代吲哚-2-酮 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学] R965[医药卫生—药学]