Résumé
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.
Résumé
OBJECTIVE: To synthesize quinolone derivatives and investigate their anti-tumor activities in vitro. METHODS: A series of quinolone derivatives were designed and synthesized from Norfloxacin or Ciprofloxacin with N-(phenylsulfonyl) formimidamide. Their anti-tumor activities in vitro were evaluated for A549, HL-60, Hela cells by MTT assay. Molecular docking studies were performed with the Discovery Studio to afford the ideal interaction mode of the compound into the binding site of the Topo I. RESULTS: Fourteen novel compounds were synthesized and the structures were characterized by H-NMR, ESI and HRMS. MTT assay showed that most quinolone derivatives exhibited some anti-tumor activities. CONCLUSION: These quinolone derivatives are worth further being developed.