Synthesis and preliminary characterization of a novel substrate for gamma-glutamyl transferase. A potential anti-hepatoma drug

Biochem Pharmacol. 1984 Feb 15;33(4):527-9. doi: 10.1016/0006-2952(84)90302-2.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aniline Mustard / analogs & derivatives
  • Aniline Mustard / chemical synthesis
  • Aniline Mustard / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology*
  • Carcinoma, Hepatocellular / drug therapy
  • Carcinoma, Hepatocellular / enzymology
  • Glutathione / metabolism
  • Humans
  • Kinetics
  • Liver Neoplasms
  • Nitrogen Mustard Compounds / pharmacology*
  • Substrate Specificity
  • gamma-Glutamyltransferase / antagonists & inhibitors*

Substances

  • Antineoplastic Agents
  • Nitrogen Mustard Compounds
  • gamma-glutamyl 4-phenylene diamine mustard
  • Aniline Mustard
  • gamma-Glutamyltransferase
  • Glutathione