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.
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. OI sindona, giovanni/0000-0002-5623-5795; ORTUSO, Francesco/0000-0001-6235-8161; ALCARO, Stefano/0000-0002-0437-358X
Molecular Modeling, Synthesis, and Preliminary Biological Evaluation of Glutathione-S-Transferase Inhibitors as Potential Therapeutic Agents
DE NINO, Antonio;SINDONA, Giovanni;
2005-01-01
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.