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Synthesis,cytotoxicity and topoisomerase II inhibitory activity of lomefloxacin derivatives |
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| Authors: | You Zhou Xiaoli Xu Yuan Sun Huaping Wang Haopeng Sun Qidong You |
| Affiliation: | 1. State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China;2. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China;3. Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China |
| Abstract: | A novel series of amide derivatives of lomefloxacin were synthesized and evaluated for their topoisomerase I and II inhibitory activity as well as cytotoxicity against a panel of five human cancer cell lines. Of the compounds prepared compounds 9d and 9g exhibited strong inhibition against topoisomerase II at 100 μM. In addition, docking studies were performed to predict the inhibition mode. |
| Keywords: | Lomefloxacin derivatives Topoisomerase I and II inhibitory activity Docking study |
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