N-甲基环丙沙星酰腙的合成及抗肿瘤活性

发布时间：2018-07-06 19:12

本文选题：氟喹诺酮 + 酰腙　；参考：《郑州大学学报(医学版)》2015年05期

【摘要】：目的:寻找转化抗菌氟喹诺酮到抗肿瘤氟喹诺酮的有效策略。方法:用酰腙作为N-甲基环丙沙星C-3羧基的生物电子等排体,合成了12个环丙沙星酰腙目标化合物,其结构经元素分析和光谱数据确证。用MTT方法评价了目标化合物体外对SMMC-7721、L1210和HL60 3种癌细胞的生长抑制活性。结果:酰腙目标物对3种实验癌细胞的生长抑制活性显著强于母体环丙沙星。构-效关系表明,苯环带吸电子化合物的活性强于供电子化合物的活性,尤其带羧基和磺酰胺基化合物的活性强于其他取代基化合物的活性。结论:氟喹诺酮C-3羧基并非是抗肿瘤活性所必需的药效团,被酰腙取代可提高其抗肿瘤活性。
[Abstract]:Objective: to find an effective strategy for transforming fluoroquinolone into antitumor fluoroquinolone. Methods: 12 ciprofloxacin acylhydrazone target compounds were synthesized with acyl hydrazone as N- methyl ciprofloxacin C-3 carboxylic group. Its structure was confirmed by elemental analysis and spectral data. The target compound was evaluated by MTT method in vitro to SMMC-77. The inhibitory activity of 21, L1210 and HL60 cancer cells. Results: the inhibitory activity of the acyl hydrazone target on the growth of the 3 experimental cancer cells is stronger than that of the mother ciprofloxacin. The structure-activity relationship shows that the activity of the benzene ring band absorption compounds is stronger than the activity of the electronic compounds, especially the carboxyl and sulfonamide groups are stronger than the others. Conclusion: fluoroquinolones C-3 carboxyl group is not a necessary pharmacophore. The substitution of acylhydrazone can improve its antitumor activity.
【作者单位】：郑州澍青医学高等专科学校药学系;河南大学化学生物学研究所;中国药科大学新药研究中心;
【基金】：国家自然科学基金面上项目20872028,21072045
【分类号】：R914.5;R96

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