3,3-diaryl-1,3-dihydroindol-2-ones as antiproliferatives mediated by translation initiation inhibition
| Autor: | Julia Iyasere, Han Chen, W. J. Christ, Frederick Harbinski, Yuhong Guo, Jose A. Halperin, Huseyin Aktas, Amarnath Natarajan, Yun Hua Fan |
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| Rok vydání: | 2004 |
| Předmět: |
Indoles
Stereochemistry Eukaryotic Initiation Factor-2 Antineoplastic Agents Endoplasmic Reticulum Chemical synthesis Cell Line chemistry.chemical_compound Structure-Activity Relationship Eukaryotic translation Cell Line Tumor Drug Discovery medicine Fluorescence Resonance Energy Transfer Humans Phosphorylation Cell growth Troglitazone In vitro chemistry Protein Biosynthesis Molecular Medicine Calcium Lead compound Intracellular medicine.drug |
| Zdroj: | Journal of medicinal chemistry. 47(8) |
| ISSN: | 0022-2623 |
| Popis: | A series of substituted 3,3-diphenyl-1,3-dihydro-indol-2-ones was synthesized from the corresponding isatins. The compounds were studied for cell growth inhibition mediated by partial depletion of intracellular Ca2+ stores that leads to phosphorylation of eIF2alpha. 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. |
| Databáze: | OpenAIRE |
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