SYNTHESIS AND EVALUATION OF THE ANTITUMOR-ACTIVITY OF 4,5-DIAMINO-SUBSTITUTED 1,2-BENZOQUINONES

A series of 4,5-diamino-substituted-1,2-benzoquinones were prepared fr om catechol and the corresponding secondary amines in high yield in a single step using copper complex formation to stabilize the intermedia te. The cytotoxicity of the products under various conditions was eval uated using the EMT-6 mammary carcinoma cell line, and antitumor activ ity was tested in the L1210 murine leukemia. The 4,5-diaziridinyl-1,2- benzoquinone was a more potent cytotoxic agent than diaziquone (AZQ) a nd was very effective against the L1210 leukemia. The azetidine, pyrro lidine, and diethylamine derivatives were not effective antitumor agen ts.