Design, Synthesis, Biological Evaluation, and Molecular Docking Studies of Quinolone Derivatives as Potential Antitumor Topoisomerase I Inhibitors

Kai-jun Shou; Jie Li; Yi Jin; Yan-wen Lv

doi:10.1248/cpb.c13-00040

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Design, Synthesis, Biological Evaluation, and Molecular Docking Studies of Quinolone Derivatives as Potential Antitumor Topoisomerase I Inhibitors

Kai-jun Shou, Jie Li, Yi Jin, Yan-wen Lv

著者情報

キーワード: quinolone derivative, antitumor, topoisomerase I, molecular docking

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2013 年 61 巻 6 号 p. 631-636

DOI https://doi.org/10.1248/cpb.c13-00040

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抄録

A novel series of quinolone derivatives (6a–n) were designed and synthesized, and their biological activities were evaluated as potential antitumor topoisomerase I (Top I) inhibitors. Among these compounds, 6j exhibited the most potent antitumor activities against multiple cancer cell lines. Docking simulation was performed to insert compound 6j into the crystal structure of DNA-Top I to determine the probable binding model.

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