Synthesis and evaluation of 2-substituted 1-methyl-1-(4-tolylsulfonyl)hydrazines as antineoplastic agents

Several N-2 substituted 1-methyl-1-(4-tolylsulfonyl)hydrazines were synthesized and evaluated for antineoplastic activity against the L1210 leukemia and the B16 melanoma. The most active compound to emerge from this study, 2-(methylsulfonyl)-1-methyl-1-(4-tolylsulfonyl)hydrazine, produced maximum percent T/C values with L1210 leukemia and B16 melanoma tumor bearing mice of 207 and 209, respectively. While the attachment of an aryl-, aralkyl-, or alkylsulfonyl moiety to N-2 resulted in retention of activity against both tumor systems, the corresponding benzoyl, 4-nitrobenzoyl, and (2-nitrophenyl)sulfenyl analogues only displayed activity against the L1210 leukemia.