Drug activation by gamma irradiation: a new direction for molecular design. Part I: In vitro and in vivo studies of a substituted polyaminoaryl nitrile.
The disodium salt of 4-diethyl aminophenyl-4',4''-bis(3-sulfobenzyl ethyl aminophenyl)acetonitrile was made and studied. It was found to release cyanide lineraly with exposure to ionizing radiation. When administered ip to mice, it was absorbed in significant amounts and retained its ability to cleave upon irradiation. Based upon this, we gathered evidence and proposed that it is feasible to design a non-toxic compound which when exposed to ionizing radiation would yield predictable reactive end products that would remain localized and augment the effects of irradiation upon a neoplasm.
D000097:Acetonitriles / Q000378:metabolism / Q000528:radiation effects*; D000814:Aniline Compounds / Q000378:metabolism / Q000528:radiation effects; D000818:Animals; D000970:Antineoplastic Agents; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D003486:Cyanides / Q000378:metabolism / Q000494:pharmacology*; D005260:Female; D005720:Gamma Rays; D066298:In Vitro Techniques; D051379:Mice; D008810:Mice, Inbred C57BL
D000097:Acetonitriles; D000814:Aniline Compounds; D000970:Antineoplastic Agents; D003486:Cyanides