Synthesis and preliminary characterization of a novel substrate for gamma-glutamyl transferase. A potential anti-hepatoma drug.
9he synthesis and chemical characterization of the gamma-glutamyl adduct of phenylenediamine mustard is reported. The activity of this compound, gamma-[N,N-bis(2-chloroethyl)-p-phenylenediamine]-glutamate, as a substrate for gamma-glutamyl transferase is demonstrated and compared with the activity of glutathione. The possible use of this material as a directed anti-hepatoma agent is discussed.
D000816:Aniline Mustard / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy / Q000201:enzymology; D005978:Glutathione / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D008113:Liver Neoplasms; D009588:Nitrogen Mustard Compounds / Q000494:pharmacology*; D013379:Substrate Specificity; D005723:gamma-Glutamyltransferase / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D009588:Nitrogen Mustard Compounds; C032019:gamma-glutamyl 4-phenylene diamine mustard; D000816:Aniline Mustard; D005723:gamma-Glutamyltransferase; D005978:Glutathione