摘要
以环丙沙星等5种喹诺酮药物为原料,经酯化、肼解后再与二茂铁甲醛缩合,合成出5个喹诺酮-二茂铁杂合物,用IR、NMR、HRMS等对产物结构进行确认和表征,并用MTT法、纸片扩散法分别对其抗肿瘤和抗菌活性进行研究。结果显示,所合成的喹诺酮-二茂铁杂合物对常见癌细胞的体外生长有较好的抑制活性。这一研究结果可为基于喹诺酮骨架的抗肿瘤新药的设计提供一种新思路。
Five novel ferrocene-quinolone hybrids were firstly synthesized via esterifieation, hydrazinolysis and then condensation with ferrocenecarbaldehyde. Their structures were characterized by IR, NMR and HRMS. The results indicated that the target compounds really showed strong inhibitory activity against several tumor cell lines, which would probably provide a new strategy for the design of novel antitumor drugs based on the quinolone skeleton.
出处
《广西师范大学学报(自然科学版)》
CAS
北大核心
2016年第2期111-115,共5页
Journal of Guangxi Normal University:Natural Science Edition
基金
国家自然科学基金资助项目(21362007)
药用资源化学与药物分子工程省部共建国家重点实验室基金资助项目(CMEMR2013-B02)
关键词
喹诺酮
二茂铁
杂合
抗肿瘤活性
抗菌活性
quinolone
ferrocene
hybrids
antitumor activity
antibacterial activity