Autor: |
Natarajan, A., Fan, Y.-H., Chen, H., Guo, Y., Iyasere, J., Harbinski, F., Christ, W. J., Aktas, H., Halperin, J. A. |
Zdroj: |
Journal of Medicinal Chemistry; April 2004, Vol. 47 Issue: 8 p1882-1885, 4p |
Abstrakt: |
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 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. |
Databáze: |
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