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

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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
Publication statusPublished - Apr 8 2004

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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