synthesis, antitumor activity and molecular docking of quinolone derivatives / 中国药学杂志

ABSTRACT

OBJECTIVE: To study the synthesis and antitumor activity of novel quinolone derivatives. METHODS: Based on the structure of ciprofloxacin, the objective substances were designed and synthesized according to the principle of fragmentbased drug discovery. Their anti-tumor activities in vitro were evaluated against A549, HL-60, and Hela cells by MTT assay. Molecular docking studies were performed with the Libdock protocol of Discovery Studio to afford the ideal interaction mode of the compound with the binding site of the Topo I. RESULTS: Eight novel compounds were synthesized and showed potential antitumor activities. CONCLUSION: The antitumor activities of the synthesized quinolone derivatives are worthy of further study.