Structure-activity requirements for the antiproliferative effect of troglitazone derivatives mediated by depletion of intracellular calcium

Yun Hua Fan, Han Chen, Amarnath Natarajan, Yuhong Guo, Fred Harbinski, Julia Iyasere, William Christ, Huseyin Aktas, Jose A. Halperin

Research output: Contribution to journalArticle

41 Scopus citations

Abstract

Depletion of calcium from the endoplasmic reticulum has shown to affect protein synthesis and cell proliferation. The anticancer effect of troglitazone was reported to be mediated by depletion of intracellular calcium stores resulting in inhibition of translation initiation. The unsaturated form of troglitazone displays similar anticancer properties in vitro. In this letter, we report our findings on the minimum structural requirements for both compounds to retain their calcium release and antiproliferative activities.

Original languageEnglish (US)
Pages (from-to)2547-2550
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number10
DOIs
StatePublished - May 17 2004

Keywords

  • Intracellular calcium
  • Thiazolidinediones
  • Troglitazone

ASJC Scopus subject areas

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

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