Molecular Modeling, Synthesis, and Preliminary Biological Evaluation of Glutathione-S-Transferase Inhibitors as Potential Therapeutic Agents

Changes in the GSH/GST system have been found to correlate with resistance to anticancer alkylating agents, presumably through accelerated detoxification of these drugs since some GSTs have been shown to catalyze the conjugation of GSH to specific antineoplastic agents. GSH-alkyl derivatives were de...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2005-09, Vol.48 (19), p.6084-6089
Main Authors: Procopio, Antonio, Alcaro, Stefano, Cundari, Sante, De Nino, Antonio, Ortuso, Francesco, Sacchetta, Paolo, Pennelli, Alfonso, Sindona, Giovanni
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
Catalytic Domain
Ethylene Oxide - analogs & derivatives
Ethylene Oxide - chemical synthesis
Ethylene Oxide - chemistry
General aspects
Glutathione - analogs & derivatives
Glutathione - chemical synthesis
Glutathione - chemistry
Glutathione Transferase - antagonists & inhibitors
Glutathione Transferase - chemistry
Humans
Medical sciences
Miscellaneous
Models, Molecular
Pharmacology. Drug treatments
Quantitative Structure-Activity Relationship
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Summary:Changes in the GSH/GST system have been found to correlate with resistance to anticancer alkylating agents, presumably through accelerated detoxification of these drugs since some GSTs have been shown to catalyze the conjugation of GSH to specific antineoplastic agents. GSH-alkyl derivatives were designed by molecular modeling, synthesized, and tested as inhibitors of human GST-Pi.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm0504609