3,3-Diaryl-1,3-dihydroindol-2-ones as Antiproliferatives Mediated by Translation Initiation Inhibition
Amarnath Natarajan(Harvard University), Yun-Hua Fan(Harvard University), Han Chen(Harvard University), Yuhong Guo(Harvard University), Julia Iyasere(Harvard University), Frederick Harbinski(Harvard University), William J. Christ(Harvard University), Hüseyin Aktaş(Harvard University), José A. Halperin(Harvard University)
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Abstract
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.
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