1-苯基-4-取代酞嗪衍生物合成及抗肿瘤活性评价（英文）

Synthesis and Antitumor Activity of 1-Phenyl-4-substituted Phthalazine Derivatives

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~1 H 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9.31μmol·L^(-1).

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 ~1 H NMR, ^（13） C 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（5 f） and N-（3-chloro-4-fluorophenyl）-2-（4-（4-phenylphthalazin-1-yl）piperazin-1-yl）acetamide（8 c）, 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.