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

Hiroyuki Miyachi, Asuka Ogasawara, Akihiko Azuma, Yuichi Hashimoto

Research output: Contribution to journalArticle

62 Citations (Scopus)

Abstract

N-Substituted phthalimides (2-substituted 1H-isoindole-1,3-diones) were prepared and their inhibitory effects on tumor necrosis factor-alpha (TNF-α) 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-α 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.

Original languageEnglish
Pages (from-to)2095-2102
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume5
Issue number11
DOIs
Publication statusPublished - Nov 1997
Externally publishedYes

Fingerprint

Structure-Activity Relationship
Okadaic Acid
Leukemia
Tumor Necrosis Factor-alpha
Tetradecanoylphorbol Acetate
Phthalimides
Acetates
Isoindoles
Cell Extracts
Carrier Proteins
Gels
Cells
Cell Line
Molecules
phthalimide

Keywords

  • Biological response modifier
  • Phthalimide
  • Phthalimide-binding protein
  • Thalidomide
  • Tumor necrosis factor-alpha

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Tumor necrosis factor-alpha production-inhibiting activity of phthalimide analogues on human leukemia THP-1 cells and a structure-activity relationship study. / Miyachi, Hiroyuki; Ogasawara, Asuka; Azuma, Akihiko; Hashimoto, Yuichi.

In: Bioorganic and Medicinal Chemistry, Vol. 5, No. 11, 11.1997, p. 2095-2102.

Research output: Contribution to journalArticle

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