4.3 Article

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

Journal

CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 61, Issue 6, Pages 631-636

Publisher

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

Keywords

quinolone derivative; antitumor; topoisomerase I; molecular docking

Funding

  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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