郑州大学学报（医学版）Issue(5)：597-601,5.DOI:10.13705/j.issn.1671-6825.2015.05.002
N-甲基环丙沙星酰腙的合成及抗肿瘤活性
Synthesis and antitumor activity of N-methyl ciprofloxacin acylhydrazone
摘要
Abstract
Aim:To explore an efficient strategy for a transformation of antibacterial fluoroquinolone into antitumor flu -oroquinolones .Methods:An acylhydrazone used as bioisostere of the C-3 carboxylic group ,twelve novel fluoroquinolone C-3 acylhydrazones were synthesized from ciprofloxacin ,respectively .The structures of the title compounds were characterized by elemental analysis and spectral data , and the in vitro antitumor activity against SMMC-7721 , L1210 and HL60 cells were also evaluated by MTT assay .Results: The title compounds exhibited more significantly inhibitory activity than the parent.The SAR showed that some title compounds with electron-withdrawing groups had more potent cytotoxicity than that of compounds with electron-donating group .In particular , some compounds bearing carboxylic group and sulfonamide group had better activity than other title compounds .Conclusion:It appears to be not necessary for the C-3 carboxylic group to develop antitumor fluoroquinolones ,and the bioisosteric replacement with a acylhydrazone group could improve the antitumor activity.关键词
氟喹诺酮/酰腙/生物电子等排体/抗肿瘤活性Key words
fluoroquinolone/acylhydrazone/bioisostere/antitumor activity分类
医药卫生引用本文复制引用
尚慧杰,高留州,谢玉锁,闫强,吴书敏,倪礼礼,黄文龙,谢松强,胡国强..N-甲基环丙沙星酰腙的合成及抗肿瘤活性[J].郑州大学学报（医学版）,2015,(5):597-601,5.基金项目
国家自然科学基金面上项目20872028，21072045 （）
