Synthesis and in vitro antitumor activity of novel naphthyridinone derivatives

A series of naphthyridinone derivatives based on la（a precursor of Voreloxin） were designed and synthesized.Seven compounds having 〉70%inhibition against HL60 at 30 μmol/L were further evaluated for their in vitro antitumor activity by SRB assay.Results reveal that thiazol-2-yl and 3-aminomethyl-4-benzyloxyimino-3-methylpyrrolidin-l-yl groups are optimal at the N-1 and C-7positions of naphthyridinone core,respectively.10 j exhibits broad-spectrum activity（IC_（50）：〈0.5-6.25 μmol/L） against all of the tested cell lines including Etoposide- and/or la-resistant ones,and is 1.3-fold to 〉100-fold more potent than the two references against eight of these cell lines.