公开(公告)号：US20040063640A1

公开(公告)日：2004-04-01

申请号：US10246424

申请日：2002-09-19

Applicant: UNIVERSITEIT LEIDEN

Inventor： Danny Burg ,  Gerard Johan Mulder

IPC: A61K038/05 ,  A61K038/04 ,  C07K005/06 ,  C07K005/04 ,  C07D213/55

CPC classification number: C07D213/32 ,  A61K38/06 ,  A61K38/063 ,  C07K5/0606 ,  C07K5/0819

Abstract: The invention relates to peptidomimetic compounds with formula 1 wherein ZnullCH2 and YnullCH2, or ZnullO and YnullCnullC), which are novel analogs of glutathion and are inhibitors of glutathione S-tansferase, in particular of GST P1-1. Such inhibition has beneficial effects in therapy against cancer. In particular compounds in which R3 is H, R4 is benzyl and R5 is phenyl are stable towards nullGT activity and are selective for GST P1-1.

Abstract translation: 本发明涉及具有下式的拟肽化合物，其中Z = CH 2和Y = CH 2，或Z = O和Y = C = C），其是谷胱甘肽的新型类似物，并且是谷胱甘肽S-转移酶的抑制剂，特别是GST P1- 1。 这种抑制在治疗癌症方面具有有益的作用。 特别是其中R 3为H，R 4为苄基且R 5为苯基的化合物对γGT活性稳定，对GST P1-1具有选择性。