类查尔酮氟喹诺酮衍生物的合成及抗肿瘤活性  

Syntheses and Antitumor Activities of Chalcone-Like Fluoroquinolone Derivatives from Pefloxacin

作　　者：冯亚莉 李珂 黄文龙[3] 崔红艳 胡国强 Feng Yali;Li Ke;Huang Wenlong;Cui Hongyan;Hu Guoqiang(Water Environment and Health Henan Engineering Technology Research Center,Zhengzhou University of Industrial Technology,Zhengzhou,451150;School of Clinical Medicine,Henan University,Kaifeng,475001;Centre of Drug Discovery,China Pharmaceutical University,Nanjing,210009)

机构地区：[1]郑州工业应用技术学院河南省水环境与健康工程技术研究中心,郑州451150 [2]河南大学临床医学院,开封475001 [3]中国药科大学新药研究中心,南京210009

出　　处：《化学通报》2022年第4期485-489,共5页Chemistry

基　　金：国家自然科学基金项目(20872028,21072045)资助。

摘　　要：基于α,β-不饱和酮的结构特征,设计合成了12个新的类查尔酮氟喹诺酮目标化合物5a~5l,其结构经元素分析和光谱数据确证,评价了它们对SMMC-7721、Capan-1和HL60三种癌细胞株的体外抗增殖活性。目标化合物的抗肿瘤活性显著高于母体化合物1,其中含氯苯基的化合物5k的活性与对照抗肿瘤药阿霉素相当。具有α,β-不饱和酮结构片段的类查尔酮氟喹诺酮化合物的抗肿瘤活性值得进一步研究。Based on the structural features of α,β-unsaturated ketones, 12 novel chalcone-like fluoroquinolone target compounds(5 a~5 l) were designed and synthesized, and their structures were determined by elemental analysis and spectroscopic data. The in vitro antiproliferative activities of as-synthesized compounds against three cancer cell lines, SMMC-7721, Capan-1 and HL60, were evaluated. Their antitumor activities were significantly higher than the parent compound 1, and the activity of compound 5 k containing chlorophenyl was comparable to that of the control anti-tumor drug doxorubicin. The antitumor activity of chalcone-like fluoroquinolone compounds with α,β-unsaturated ketone structural fragments deserves further investigation.

关 键 词：氟喹诺酮 Α Β-不饱和酮 类查尔酮 抗肿瘤活性 

分 类 号：TQ460.1[化学工程—制药化工]