摘要/Abstract

为了找到更有效和更经济的抗肿瘤药物，合成了一系列1-苯基-4-取代酞嗪衍生物，并评估了其体外抗增殖活性.所合成的化合物的结构都通过¹H NMR，¹³ C NMR和HRMS确证.并且通过3-（4，5-二甲基噻唑-2）-2，5-二苯基四氮唑溴盐（MTT）法评估了目标化合物对四种人类癌细胞株的抗肿瘤活性.结果表明：一些化合物具有良好的抗肿瘤活性，特别是N-（4-甲氧基苯基）-2-（（4-苯基酞嗪-1-基）硫基）乙酰胺（5f）和N-（3-氯-4-氟苯基）-2-（4-（4-苯基酞嗪-1-基）哌嗪-1-基）乙酰胺（8c）表现出了更好的抗肿瘤活性，对人类食管癌细胞的活性优于5-氟尿嘧啶.IC₅₀值分别为8.13和9.31 μmol·L^－1.
关键词: 合成, 酞嗪衍生物, 抗肿瘤活性
In order to find more efficient and economical antitumor drugs, a series of 1-phenyl-4-substituted phthalazine derivatives were synthesized and evaluated for antiproliferative activity in vivo. The structures of the synthesized compounds were confirmed by ¹H NMR, ¹³C NMR and HRMS. The antitumor activity of the target compounds was performed against four cancer cell lines by 3-(4, 5-dimethyl-2-thiazolyl)-2, 5-diphenyl-2-H-tetrazolium bromide (MTT). The results showed that some compounds had a good antitumor activity, especially, N-(4-methoxyphenyl)-2-((4-phenylphthalazin-1-yl) thio) acetamide (5f) and N-(3-chloro-4-fluorophenyl)-2-(4-(4-phenylphthalazin-1-yl) piperazin-1-yl) acetamide (8c), exhibited better antitumor activities with IC₅₀ values of 8.13 and 9.31 μmol•L^-1 against the human esophageal cancer cells, which were superior to 5-fuorouracil.
Key words: synthesis, phthalazine derivative, antitumor activity


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