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为发现新型抗肿瘤绕丹宁不饱和酮衍生物,以氟喹诺酮酰胺骨架作为载体,设计合成了氟喹诺酮(绕丹宁α,β-不饱和酮)酰胺类目标化合物5a~5r,其结构经元素分析、1H NMR、MS确证。采用MTT法评价了目标化合物对人肝癌Hep-3B细胞、人Capan-1胰腺癌细胞及人HL60白血病细胞的体外增值抑制活性。结果表明,18个目标化合物对3种实验癌细胞的抗增殖活性均显著高于母体环丙沙星1的活性,其中对Capan-1细胞的活性最强,尤其是芳杂环或苯环带有吸电子羧基及磺酰氨基类化合物的活性与对照抗肿瘤药物阿霉素相当。为此,氟喹诺酮(绕丹宁不饱和酮)酰胺衍生物是一类有发展前景的抗肿瘤活性先导物。
In order to find novel antitumor rhodanine unsaturated ketone derivatives, the target compounds 5a ~ 5r of fluoroquinolone (rhodanine α, β-unsaturated ketone) amide were designed and synthesized by using fluoroquinolone amide as carrier. The structure of Elemental analysis, 1H NMR, MS confirmatory. The inhibitory activity of the target compound against human hepatoma Hep-3B cells, human Capan-1 pancreatic cancer cells and human HL60 leukemia cells was evaluated by MTT assay. The results showed that the antiproliferative activity of 18 target compounds was significantly higher than that of maternal ciprofloxacin 1 in three kinds of experimental cancer cells, of which Capan-1 cells were the most active, especially aromatic heterocycle or benzene ring The electron-withdrawing carboxyl and sulfonamido compounds are comparable in activity to the control antitumor drug doxorubicin. To this end, fluoroquinolone (rhodanine unsaturated ketone) amide derivatives is a class of promising antitumor activity leader.