Use of 7-nitro-2,1,3-benzoxadiazole derivatives for anticancer therapy

摘要

Derivatives of the heterocyclic compound known as 7-nitro-benzofurazan or 7-nitro-2,1,3-benzoxadiazole, are agents having a strong inhibiting activity towards members of the glutathione S-transferase (GST) superfamily that are hyperexpressed in cancer cells, and make them particularly resistant to many stress factors. These compounds are useful in the production of pharmaceutical drugs to be used in anticancer therapy, and may be employed either alone or in combination with other chemotherapeutic agents.

主权项

1. A method of inhibiting glutathione S-transferase (GST) enzyme in the treatment of cancer, which method comprises: administering to a patient in need thereof an effective amount of a derivative of 7-nitro-2,1,3-benzoxadiazole of the formula:wherein R1 is a linear, branched or cyclic alkyl with up to 12 carbon atoms, one hydrogen atom of R1 being optionally substituted with one group selected from the group consisting of OR2, NO2, and NR2R3, wherein R2 and R3 are each independently selected from the group consisting of H, linear, branched or cyclic alkyl and alkenyl or alkynyl with up to 12 carbon atoms, and wherein said S—R1 group is not a good leaving group.