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5H-苯并[b]咔唑类化合物的合成与肿瘤细胞增殖抑制活性

曹素芬, 谢琴, 陈奕, 段文虎

曹素芬, 谢琴, 陈奕, 段文虎. 5H-苯并[b]咔唑类化合物的合成与肿瘤细胞增殖抑制活性[J]. 中国药科大学学报, 2017, 48(2): 157-166. DOI: 10.11665/j.issn.1000-5048.20170205
引用本文: 曹素芬, 谢琴, 陈奕, 段文虎. 5H-苯并[b]咔唑类化合物的合成与肿瘤细胞增殖抑制活性[J]. 中国药科大学学报, 2017, 48(2): 157-166. DOI: 10.11665/j.issn.1000-5048.20170205
CAO Sufen, XIE Qin, CHEN Yi, DUAN Wenhu. Synthesis and antiproliferative activities of 5H-benzo[b]carbazole-6, 11-diones[J]. Journal of China Pharmaceutical University, 2017, 48(2): 157-166. DOI: 10.11665/j.issn.1000-5048.20170205
Citation: CAO Sufen, XIE Qin, CHEN Yi, DUAN Wenhu. Synthesis and antiproliferative activities of 5H-benzo[b]carbazole-6, 11-diones[J]. Journal of China Pharmaceutical University, 2017, 48(2): 157-166. DOI: 10.11665/j.issn.1000-5048.20170205

5H-苯并[b]咔唑类化合物的合成与肿瘤细胞增殖抑制活性

基金项目: 中国科学院上海药物研究所自主部署基金资助项目(No.CASIMM0120152005,No.CASIMM0120151011);中国科学院战略性先导科技专项资助(No.XDA012020303)

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

  • 摘要: 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HeLa)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(IC50分别为:5.06,4.50,5.29和6.32 μmol/L)。
    Abstract: 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.
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  • 刊出日期:  2017-04-24

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