4.3 Article

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

期刊

CHEMICAL & PHARMACEUTICAL BULLETIN
卷 61, 期 6, 页码 631-636

出版社

PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c13-00040

关键词

quinolone derivative; antitumor; topoisomerase I; molecular docking

资金

  1. Natural Science Foundation of Zhejiang Province [Y2100908]

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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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