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

ABSTRACT

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.