1,2-bis(arylsulfonyl)hydrazines. 2. The influence of arylsulfonyl and aralkylsulfonyl substituents on antitumor and alkylating activity.

Abstract

Several 1,2-bis(arylsulfonyl)-1-methylhydrazines were synthesized and evaluated for antineoplastic activity against the L1210 leukemia. The most active compound to emerge from this study, 2-[(4-chlorophenyl)sulfonyl]-1-methyl-1-(4-tolylsulfonyl)hydrazine , increased the survival time of tumor-bearing mice by 88%. The alkylating activity of the synthesized analogues and several compounds reported earlier was determined by measuring the absorbance at 540 nm of the alkylated product of 4-(4-nitrobenzyl)pyridine. The results obtained support the concept that the ability to alkylate is a necessary but not a sufficient condition for the expression of antitumor activity by agents of this class.

• Authors: K Shyam, R Furubayashi, R T Hrubiec, L A Cosby, A C Sartorelli
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 29 Issue 7 Pg. 1323-5 (Jul 1986) ISSN: 0022-2623 [Print] United States
• PMID: 3806585 (Publication Type: Comparative Study, Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Alkylating Agents
• Antineoplastic Agents
• Hydrazines
• Indicators and Reagents

Topics

• Alkylating Agents (chemical synthesis)
• Alkylation
• Animals
• Antineoplastic Agents (chemical synthesis)
• Drug Evaluation, Preclinical
• Hydrazines (chemical synthesis, pharmacology)
• Indicators and Reagents
• Leukemia L1210 (drug therapy)
• Magnetic Resonance Spectroscopy
• Mice
• Structure-Activity Relationship