Abstract Coumarin and its nitrogen analogue 1-aza coumarin are a class of lactones and lactams, respectively, which are indispensable heterocyclic units to both chemists and biochemists. 1-Aza coumarin derivatives, which ultimately metabolize as the corresponding 8-hydroxy coumarins in the biological system are therefore found to be very good anti-inflammatory, anti-cancer, and analgesic agents. A series of hybrid substituted coumarin and azacoumarin-3-carboxylic acid derivatives (8-methoxycoumarin-3-carboxylic acid (4a), 8-methoxyazacoumarin-3-carboxylic acid (4b), 5-bromo-8-methoxycoumarin-3-carboxylic acid (5a), 5-bromo-8-methoxyazacoumarin-3-carboxylic acid (5b), 2-acetoxy-5-bromo-8-methoxyquinoline-3-carboxylic acid (6), and 5,7-di(phenylazo)-8-methoxycoumarin-3-carboxylic acid (7) were synthesized and structurally proved using spectral and elemental analysis data. Substituted coumarin-3-carboxylic acid (4a and 5a) and Substituted azacoumarin-3-carboxylic acid (4b, 5b and 6) were tested for their in vitro cytotoxic activity against MCF-7 and HepG-2 cell lines.

中文翻译：

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一些香豆素和氮杂香豆素衍生物的合成及抗癌评价

摘要 香豆素及其氮类似物1-氮杂香豆素分别是一类内酯类和内酰胺类，是化学家和生物化学家不可缺少的杂环单元。因此，发现在生物系统中最终代谢为相应的 8-羟基香豆素的 1-氮杂香豆素衍生物是非常好的抗炎、抗癌和镇痛剂。一系列杂化取代香豆素和氮杂香豆素-3-羧酸衍生物（8-甲氧基香豆素-3-羧酸（4a）、8-甲氧基氮杂香豆素-3-羧酸（4b）、5-溴-8-甲氧基香豆素-3-羧酸酸(5a)、5-溴-8-甲氧基氮香豆素-3-羧酸(5b)、2-乙酰氧基-5-溴-8-甲氧基喹啉-3-羧酸(6)和5，使用光谱和元素分析数据合成并证明了 7-二（苯基偶氮）-8-甲氧基香豆素-3-羧酸 (7)。测试了取代的香豆素-3-羧酸（4a 和 5a）和取代的氮杂香豆素-3-羧酸（4b、5b 和 6）对 MCF-7 和 HepG-2 细胞系的体外细胞毒活性。