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.
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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.)
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Chemical References |
- Alkylating Agents
- Antineoplastic Agents
- Hydrazines
- Indicators and Reagents
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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
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