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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.
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 as their in vitro antitumor activity by SRB assay. Results reveal that thiazol -2-yl and 3-aminomethyl-4-benzyloxyimino-3-methylpyrrolidin-1-yl groups are optimal at the N-1 and C-7 positions of naphthyridinone core, : <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.