【摘要】 目的 设计合成新型甲氧基咔唑类抗肿瘤化合物。方法 将4,5-二甲氧基-2-溴硝基苯与甲氧基碘代苯化合物在铜粉催化下经Ullmann反应制得甲氧基-硝基联苯化合物,再经亚磷酸三乙酯还原得三种甲氧基咔唑。对9-位氮进行修饰,合成了16个衍生物。利用核磁共振、质谱、红外光谱和元素分析进行了结构确认。结果 体外初步抗肿瘤活性测试结果显示,目标物4c,5a,5b,5g,5h,5i,5l,5n和5p对人结肠癌HT-29细胞的IC50值分别12.1,10.6,8.1,3.1,4.4,10.1及9.2μmol·L～1。目标物4a对人口腔上皮癌KB细胞的IC50值为17.7μmol·L～1。结论 部分目标化合物对HT-29及KB肿瘤细胞具有较好的抑制作用。更多还原

【Abstract】 Aim To design and synthesize new methoxyl carbazole analogues as antitumor compounds. Methods Methoxyl-nitrobiphenyls (3a -3c) were prepared through the Ullmann reaction of 4,5-dimethoxyl-2-bromonitrobenzene and methoxyl-iodobenzene compounds with the catalysis of copper powder, and then reduced by P(EtO)3 to obtain methoxyl carbazoles 4a -4c. The modification at 9-position of the methoxyl carbazoles (4a -4c) gives 16 carbazole derivatives (5a -5p). These compounds were confirmed by 1HNMR, MS, IR and elemental analysis. Result In vitro antitumor activities evaluation in vitro demonstrated that IC50 value of the target compounds 4c, 5a, 5b, 5g, 5h, 5i, 5l, 5n and 5p against HT -29 cells were 12. 1, 10. 6, 8. 1, 3. 1, 4. 4, 10. 1 and 9. 2 μmol · L-1 respectively, and IC50 value of the target compound 4a against KB was 17. 7 μmol · L-1. Conclusion Some of the target compounds have better inhibitory effects against H-29 and KB cells.更多还原