Novel biological response modifiers: phthalimides with tumor necrosis factor-alpha production-regulating activity.
Novel N-substituted phthalimides (2-substituted 1H-isoindole-1,3-diones) were prepared, and their effects on tumor necrosis factor-alpha (TNF-alpha) production by human leukemia cell line HL-60 stimulated with 12-O-tetradecanoylphorbol 13-acetate (TPA) or okadaic acid (OA) were examined. A structure-activity relationship study of the N-phenylphthalimides and N-benzylphthalimides revealed that their enhancing effect on TPA-induced TNF-alpha production by HL-60 cells and their inhibiting effect on OA-induced TNF-alpha production by HL-60 cells are only partially correlated.
Miyachi
H
H
Institute of Molecular and Cellular Biosciences, University of Tokyo, Japan.
Azuma
A
A
Ogasawara
A
A
Uchimura
E
E
Watanabe
N
N
Kobayashi
Y
Y
Kato
F
F
Kato
M
M
Hashimoto
Y
Y
D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D018922:HL-60 Cells / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D007155:Immunologic Factors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D019319:Okadaic Acid / Q000494:pharmacology; D009904:Optical Rotation; D010797:Phthalimides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000096:biosynthesis*
D007155:Immunologic Factors; D010797:Phthalimides; D014409:Tumor Necrosis Factor-alpha; D019319:Okadaic Acid; D013755:Tetradecanoylphorbol Acetate