Molecular modeling, synthesis, and preliminary biological evaluation of glutathione-S-transferase inhibitors as potential therapeutic agents

被引：11

作者：

Procopio, A

Alcaro, S

Cundari, S

De Nino, A

Ortuso, F

Sacchetta, P

Pennelli, A

Sindona, G

机构：

[1] Magna Graecia Univ Catanzaro, Dipartimento Sci Farmacobiol, I-88021 Roccelleta Di Borgia, CZ, Italy

[2] Univ Calabria, Dipartimento Chim, I-87036 Arcavacata Di Rende, CS, Italy

[3] Sigma Tau Ifr SpA, R&D Dept, I-00040 Pomezia, Rome, Italy

[4] Univ G DAnnunzio, Dipartimento Sci Biomed, I-65100 Chieti, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 19期

关键词：

D O I：

10.1021/jm0504609

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

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页码：6084 / 6089

页数：6

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