| 冯亚莉,李珂,黄文龙,崔红艳,胡国强.化学通报,2022,85(4):485-489. |
| 类查耳酮氟喹诺酮衍生物的合成及抗肿瘤活性 |
| Synthesis and antitumor activity of chalcone-like fluoroquinolone derivatives from pefloxacin |
| 投稿时间：2021-07-26 修订日期：2021-09-06 |
| DOI： |
| 中文关键词: 氟喹诺酮 α，β-不饱和酮 类查耳酮 抗肿瘤活性 |
| 英文关键词:fluoroquinolone α,β-unsaturated ketone chalcone-like antitumor activity |
| 基金项目: |
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| 中文摘要: |
| 目的 发现氟喹诺酮由抗菌活性向抗肿瘤活性转化的有效结构修饰策略。方法 基于α，β-不饱和酮的结构特征,设计合成了12个新的类查耳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。结果目标化合物的抗肿瘤活性显著高于母体化合物1,其中氯苯基化合物(5k)的活性与对照抗肿瘤药阿霉素相当。结论 具有a,b-不饱和酮结构片段的类查耳酮氟喹诺酮化合物的抗肿瘤活性值得进一步研究。 |
| 英文摘要: |
| Objective To discover effective structural modification strategies for the conversion of fluoroquinolones from antibacterial activity to antitumor activity. Methods Based on the structural features of α,β-unsaturated ketones, 12 novel chalcone-like fluoroquinolone target compounds (5a~5l) were designed and synthesized. The structures of the target compounds were determined by elemental analysis and spectroscopic data, and their in vitro antiproliferative activities against three cancer cell lines, SMMC-7721, Capan-1 and HL60, were evaluated. Results Compared to the parent pefloxacin 1, The antitumor activity of the target compounds was significantly higher than the parent compound 1, where the activity of the chlorophenyl compound (5k) was comparable to that of the control antitumor agent adriamycin. Conclusion The antitumor activity of chalcone-like fluoroquinolone compounds with α,β-unsaturated ketone structural fragments deserves further investigation.. |
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