Modification of intracellular free calcium in cultured F2408 embryo fibroblasts by 3-sub substituted-2-thiohydantoin derivatives

Incesu Z., Benkli K., Akalin G., KAPLANCIKLI Z. A.

CELL BIOLOGY INTERNATIONAL, no.4, pp.267-272, 2004 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Publication Date: 2004
  • Doi Number: 10.1016/j.cellbi.2004.01.003
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.267-272
  • Keywords: thiohydantoin, intracellular Ca2+, fibroblast, toxicity, ION CHANNELS, CELL
  • Anadolu University Affiliated: Yes


3-substituted-2-thiohydantoin derivatives were synthesized and their Structures elucidated by IR, H-1-NMR spectroscopy and elemental analysis. The cytotoxicity of the 2-thiohydantoin derivatives to rat embryo fibroblasts (F2408) in vitro was determined, and the effects of these compounds on intracellular free Ca2+, [Ca2+](i) were measured by spectrofluorophotometry. Cytotoxicity was determined by metabolic reduction of a tetrazolium salt to a formazan dye (MTT assay). Compounds 4 and 7 showed cytotoxic activity, with IC50 values in the range of 1-1.2 muM. Introduction of either chlorophenyl, metoxyphenyl, nitrophenyl or benzyl groups at C-3 resulted in concentration-dependent cytotoxic effects. Compounds 1-6 at 1 muM or more significantly increased [Ca2+](i) in a dose-dependent manner in the cultured fibroblasts. This action may have been mediated through intracellular calcium stores. (C) 2004 Elsevier Ltd. All rights reserved.