A series of 2,3,4,9-tetrahydrofuro[2,3-b]quinolin-3,4-dione and ethyl 2-(substituted aniline) -4-oxo-4,5-dihydrofuran-3-carboxylate were synthesized and evaluated for cytotoxicity on murine leukemia WEHI-3 cells. The cytotoxic effects of most compounds tested were dose-dependent and the structure-activity relationships indicated that N-substituted benzyl derivatives displayed a stronger inhibitory activity against murine leukemia WEHI-3 cells compared to non-N-substituted benzyl substituted derivatives.