摘要/Abstract

摘要： 目的·发现以6,11-二氢-5H-苯并[a]咔唑环为母核可抑制宫颈癌细胞增殖的先导化合物。方法·用Fisher吲哚合成法制备了一系列6,11-二氢-5H-苯并[a]咔唑类化合物及其类似物，并在体外用CCK8法测试了这些化合物对HeLa细胞增殖的抑制作用。结果· 2-甲氧基-6,11-二氢-5H-苯并[a]咔唑和8-氯-2-甲氧基-6,11-二氢-5H-苯并[a]咔唑具有良好的抑制HeLa细胞增殖的活性，其半数抑制浓度（IC50）值分别为9.61 μmol/L和16.52 μmol/L。结论·发现2个目标先导化合物。在6,11-二氢-5H-苯并[a]咔唑类衍生物中，母环2位C上为甲氧基取代的衍生物具有较好的抗宫颈癌细胞增殖活性。
关键词: 6,11二氢-5H-苯并[a]咔唑类化合物, 优势结构, 宫颈癌, 先导化合物
Abstract:
Objective · To discover lead compounds with 6,11-dihydro-5H-benzo[a]carbazole as core scaffold that can inhibit the proliferation of cervical cancer cells. Methods · A series of 6,11-dihydro-5H-benzo[a]carbazole derivatives and analogs were synthesized using Fischer indole synthesis method, and their anticancer activity against HeLa cells was tested in vitroCCK8 test. Results · 2-Methoxy-6,11-dihydro-5H-benzo[a]carbazole and 8-chloro-2methoxy- 6,11-dihydro-5H-benzo[a]carbazole could significantly inhibit the proliferation of HeLa cells with the half maximal inhibitory concentration (IC50)values of 9.61 μmol/L and 16.52 μmol/L, respectively. Conclusion · Two objective lead compounds were found. Among 6,11-dihydro-5H-benzo[a]carbazole derivatives, compounds with methoxy group at the C-2 position of the core scaffold show better activity against proliferation of cervical cancer cells.
Key words: 6,11-dihydro-5H-benzo[a]carbazole analogues, privileged structure, cervical cancer, lead compound


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