Tumor necrosis factor-alpha production-inhibiting activity of phthalimide analogues on human leukemia THP-1 cells and a structure-activity relationship study

被引：63

作者：

Miyachi, H ^{[1
]}

Ogasawara, A ^{[1
]}

Azuma, A ^{[1
]}

Hashimoto, Y ^{[1
]}

机构：

[1] UNIV TOKYO,INST MOL & CELLULAR BIOSCI,BUNKYO KU,TOKYO 113,JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 11期

关键词：

tumor necrosis factor-alpha; phthalimide; thalidomide; phthalimide-binding protein; biological response modifier;

D O I：

10.1016/S0968-0896(97)00148-X

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

N-Substituted phthalimides (2-substituted 1H-isoindole-1,3-diones) were prepared and their inhibitory effects on tumor necrosis factor-alpha (TNF-alpha) production by human leukemia cell line THP-1 stimulated with 12-O-tetradecanoylphorbol 13-acetate (TPA) or okadaic acid (OA) were examined. A structure-activity relationship study of these phthalimide analogues revealed that their inhibitory effects on TPA-and OA-induced TNF-alpha production by THP-1 cells are well correlated to each other, i.e. they may involve the same target molecule(s). An analysis by the use of phthalimide analogue-immobilized affinity gels indicated the existence of several phthalimide-binding proteins in THP-1 cell extract. (C) 1997 Elsevier Science Ltd.

引用

页码：2095 / 2102

页数：8

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