5H-苯并[b]咔唑类化合物的合成与肿瘤细胞增殖抑制活性

Synthesis and antiproliferative activities of 5H-benzo[b]carbazole-6,11-diones

为了发现新型选择性拓扑异构酶Ⅱ抑制剂,以偏苯酸酐和吲哚为原料,合成了16个新的5H-苯并[b]咔唑类化合物。探讨了C-9位上了不同取代基对肿瘤细胞增殖抑制活性的影响。采用磺酰罗丹明B蛋白染色法检测了16个化合物对4种肿瘤细胞(SMMC-7721、S1、HCT116和He La)的增殖抑制活性。结果表明,其中4个化合物对4种不同的肿瘤细胞株具有明显的增殖抑制活性。其中化合物10e对4种肿瘤细胞株的抑制作用最为显著(IC_(50)分别为:5.06,4.50,5.29和6.32μmol/L)。

A series of 5H-benzo［b］carbazole derivatives were synthesized to find new TopII inhibitors. The substitution pattern at C-9 was discussed. All 16 compounds were tested for their antiproliferative activities against 4 tumor cell lines（SMMC-7721, S1, HCT116, and HeLa）by sulforhodamine B assay. Four compounds were found to inhibit the proliferation of all tested cell lines. And compound 10e displayed the best antiproliferative activity against all 4 tested cell lines with IC50 values of 5. 06, 4. 50, 5. 29, and 6. 32 μmol/L, respectively.