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 were tested in the Ames test and were not found to be mutagenic.
D000332:Aerobiosis; D000818:Animals; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D006224:Cricetinae; D003412:Cricetulus; D004307:Dose-Response Relationship, Radiation; D007202:Indicators and Reagents; D008168:Lung; D009152:Mutagenicity Tests; D009153:Mutagens; D009574:Nitro Compounds / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis*; D012486:Salmonella typhimurium / Q000187:drug effects; D013329:Structure-Activity Relationship
D007202:Indicators and Reagents; D009153:Mutagens; D009574:Nitro Compounds; D011719:Pyrazines; D011838:Radiation-Sensitizing Agents