2-(3-arylacryloyl)-3-Methylquinoxaline 1,4-Dioxides as Potential Hypoxic Selective Cytotoxins

Document Type


Publication Date



The synthesis of a series of 2-(3-arylacryloyl)-3-methylquinoxaline 1,4-dioxides is reported. In-vitro cytotoxic activity of these compounds was evaluated via the MTT assay in B16 murine melanoma and L1210 murine leukemia cell lines. A dichloro analogue was found to be the most cytotoxic and was > 30-fold more active than the quinoxaline control (IC50 = 2 vs. 67 mu M in L1210, respectively). These results suggest that compounds containing two bioactive moieties could be developed as hypoxic selective cytotoxins.