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.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002470:Cell Survival / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D006834:Hydrazines / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D007202:Indicators and Reagents; D007939:Leukemia L1210 / Q000188:drug therapy; D008546:Melanoma, Experimental / Q000188:drug therapy; D051379:Mice; D008810:Mice, Inbred C57BL; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D006834:Hydrazines; D007202:Indicators and Reagents