2-(3-arylacryloyl)-3-Methylquinoxaline 1,4-Dioxides as Potential Hypoxic Selective Cytotoxins
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.
Published in: HeterocyclicCommunications, Volume 14, Issue 5, January 1, 2008, pages 385-388. Copyright © 2008 Freund Publishing House Ltd., Tel Aviv, Israel. The final published version is available at: http://dx.doi.org/10.1515/HC.2008.14.5.385