3,3-Diaryl-1,3-dihydroindol-2-ones as Antiproliferatives Mediated by Translation Initiation Inhibition

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

Research output: Contribution to journalArticle

64 Scopus citations

Abstract

A series of substituted 3,3-diphenyl-1,3-dihydroindol-2-ones was synthesized from the corresponding isatins. The compounds were studied for cell growth inhibition mediated by partial depletion of intracellular Ca 2+ stores that leads to phosphorylation of eIF2α. The diphenyloxindole (1) showed mechanism-specific antiproliferative activity that was comparable to known translation initiation inhibitors such as clotrimazole or troglitazone. SAR studies identified m'-tert-butyl and o-hydroxy substituted diphenyloxindole (25) as a lead compound for Ca2+-depletion-mediated inhibition of translation initiation.

Original languageEnglish (US)
Pages (from-to)1882-1885
Number of pages4
JournalJournal of Medicinal Chemistry
Volume47
Issue number8
DOIs
StatePublished - Apr 8 2004

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Natarajan, A., Fan, Y. H., Chen, H., Guo, Y., Iyasere, J., Harbinski, F., Christ, W. J., Aktas, H., & Halperin, J. A. (2004). 3,3-Diaryl-1,3-dihydroindol-2-ones as Antiproliferatives Mediated by Translation Initiation Inhibition. Journal of Medicinal Chemistry, 47(8), 1882-1885. https://doi.org/10.1021/jm0499716