Anticancer anthrapyrazoles. The synthesis of 2-substituted 5-nitro and 5-aminoanthra[1,9-cd]pyrazol-6(2H)-ones

Synthetic methodologies for the preparation of substituted 5-nitro- and 5-aminoanthra[1,9-cd]-pyrazol-6(2H)-ones, 4 and 5 respectively, substituted with a basic side at N-2 and dioxy substitution in the A-ring, are reported. These compounds are essentially devoid of activity against in vitro L1210 leukemia and in vivo murine P388 leukemia.