中文摘要：

目的观察3-取代芳基氧化吲哚（PHⅡ-7）在肿瘤细胞内的定位。方法通过化学合成的方法，在PHⅡ-7的1位引入氨烷基侧链，并将其氨基端进行FITC衍生化，在进行此衍生物体外抗肿瘤活性测定后，用激光共聚焦成像技术进行其在肿瘤细胞内的定位。结果成功合成具有氨烷基侧链的PHⅡ-7衍生物，并使之与FITC偶联；合成衍生物具有一定体外抗肿瘤活性；随着PHⅡ-7作用时间的增加，药物在肿瘤细胞系K562及其耐药肿瘤细胞系K562／A02中均逐渐由细胞质向细胞核内聚集。结论对于肿瘤细胞系K562及其耐药肿瘤细胞系K562／A02，PHⅡ-7作用靶位均为细胞核。

英文摘要：

Aim To study the intracellular location of 3-subsittuted aryl oxindole （ PHⅡ -7 ） in tumor cells. Methods The derivative with amino-alkyl side chain at I site of PHⅡ-7 was synthesized and linked with FITC by organic chemistry approaches, and its in vitro activity was evaluated using human leukemic cell line K562 cell and its MDR subline K562/A02 cell in order to identify the intracellular location of PH Ⅱ-7 with eonfocal microscope. Results The derivative with amino-alkyI side chain in PH Ⅱ-7 was synthesized and linked with FITC successfully. The derivative inhibited the proliferation of leukemic K562 and its MDR subline K562/A02 cells. The main distribution locations of PH Ⅱ-7 changed from cytoplasm to nuclear as time passed in both human leukemic K562 and its MDR subline K562/A02 cells when observed with confocal microscope. Conclusion The target sites in which PH Ⅱ-7 takes function are nuclear in both human leukemic K562 and its MDR subline K562/A02 cells.