Synthesis and activity of novel nitropyrazines for use as hypoxic cell radiosensitizers

A series of eight novel nitropyrazines has been prepared by oxidation of sulfoximine intermediates. The partition coefficient, one-electron reduction potential, sensitizer enhancement ratio, and chronic and acute aerobic cytotoxicity have been measured for each. Two representatives of this series we...

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Veröffentlicht in:	Journal of medicinal chemistry 1984-12, Vol.27 (12), p.1634-1639
Hauptverfasser:	Hartman, George D, Hartman, Richard D, Schwering, John E, Jones, Nigel R, Wardman, Peter, Watts, Margaret E, Woodcock, Michael
Format:	Artikel
Sprache:	eng
Schlagworte:	Aerobiosis Animals Cell Line Cell Survival - drug effects Cell Survival - radiation effects Chemistry Cricetinae Cricetulus Dose-Response Relationship, Radiation Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings Indicators and Reagents Lung Mutagenicity Tests Mutagens Nitro Compounds - chemical synthesis Nitro Compounds - pharmacology Nitro Compounds - toxicity Organic chemistry Preparations and properties Pyrazines - chemical synthesis Pyrazines - pharmacology Pyrazines - toxicity Radiation-Sensitizing Agents - chemical synthesis Salmonella typhimurium - drug effects Structure-Activity Relationship
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Zusammenfassung:	A series of eight novel nitropyrazines has been prepared by oxidation of sulfoximine intermediates. The partition coefficient, one-electron reduction potential, sensitizer enhancement ratio, and chronic and acute aerobic cytotoxicity have been measured for each. Two representatives of this series were tested in the Ames test and were not found to be mutagenic.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00378a018