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Citation: Shen Ruizhi, Zeng Tianying, Zhang Haihui, Huang Wenlong, Hu Guoqiang. Syntheses and Antitumor Activities of Fluoroquinolone-3-N-Amide Derivatives[J]. Chemistry, ;2020, 83(8): 730-734. shu

Syntheses and Antitumor Activities of Fluoroquinolone-3-N-Amide Derivatives

1.
College of pharmacy, Henan University, Kaifeng, 475001
2.
College of Chemistry and Molecular Sciences, Wuhan University, Wuhan, 430070
3.
Xinke College, Henan Institute of Science and Technology, Xinxiang, 453003
4.
Center for Drug Discovery, China Pharmaceutical University, Nanjing, 210009
5.
Institute of Drugs, Henan University, Kaifeng, 475001

Corresponding author: Hu Guoqiang, hgqxy@sina.com
Received Date: 2 March 2020
Accepted Date: 20 March 2020

Figures(1)

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.
- Fluoroquinolone,
- Amide group,
- Bioelectron isosteric,
- Antitumor activity
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