| 沈睿智,曾天映,张海惠,黄文龙,胡国强.化学通报,2020,83(8):730-734. |
| 氟喹诺酮-3-N-酰胺类衍生物的合成与抗肿瘤活性 |
| Syntheses and Antitumor Activities of Fluoroquinolone-3-N-Amide Derivatives |
| 投稿时间：2020-03-02 修订日期：2020-03-20 |
| DOI： |
| 中文关键词: 氟喹诺酮 酰胺 生物电子等排 抗肿瘤活性 |
| 英文关键词:Fluoroquinolone Amide group Bioelectron isosteric Antitumor activity |
| 基金项目:国家自然科学基金项目（20872028，21072045）和河南省科技发展计划项目（162102310392）资助 |
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| 中文摘要: |
| 为扩展氟喹诺酮由抗菌活性向抗肿瘤活性转化的结构修饰策略，利用药效团生物电子等排及其拼合和骨架迁越药物化学分子构建方法，以酰胺基作为氟喹诺酮C-3位羧基的生物电子等排体，氟喹诺酮骨架为酰胺基的功能修饰基，设计合成了氟喹诺酮-3-N-酰胺类目标化合物。其结构经元素分析和光谱数据确证。体外抗肿瘤实验结果表明，目标化合物对Hep-3B细胞和Capan-1细胞的抗增殖活性均显著强于母体环丙沙星的活性，尤其对Hep-3B细胞的抑制活性最强。因此，用酰胺基来替代C-3羧基有利于提高氟喹诺酮的抗肿瘤活性。 |
| 英文摘要: |
| To expand an efficient strategy for the conversion of antibacterial activity of fluoroquinolones into an antitumor activity, utilizing pharmacophore bioelectronics isosteric and its flattening and skeleton migration medicinal molecule construction method, a series of fluoroquinolone-3-N-amide compounds were synthesized by using amide group as the bioisostere of the fluoroquinolone C-3 carboxyl group and fluoroquinolone skeleton as a functional modification group, and their structures are confirmed by elemental analysis and spectral data. The results of in vitro antitumor activity showed that the anti-proliferative activity of the target compounds against the two experimental tumor cells (Hep-3B、Capan-1) was significantly stronger than that of the raw material ciprofloxacin, suggesting that replacing the C-3 carboxyl group with an amide group is beneficial to improve the antitumor activity of the quinolones, which provides a new structural modification pathway for transforming antibacterial activity of fluoroquinolone to antitumor activity. |
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