Journal of Medicinal Chemistry · 2004 · 187 citations · 8 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryMolecular OncologyStructure-activity RelationshipsLung Cancer PharmacotherapyOncology PharmacologyAnticancer ActivityAnticancer ChemotherapyAnticancer Mechanism Of ActionCalcium Release From Intracellular StoresCancer Cell Proliferation InhibitionSubstitution Pattern Analysis
Structure-activity relationship studies of substituted arylsulfoanilides as antiproliferatives, which are mediated by the partial depletion of intracellular Ca(2+) stores, resulted in the identification of compounds with micromolar activity against lung cancer cells in a growth inhibition assay. Incorporating the substitution pattern of the best arylsulfoanilides onto the 3-phenyloxindole scaffold resulted in a potent arylsulfoanilide-oxindole hybrid, 27. Compound 27 inhibits cancer cell growth by partial depletion of intracellular Ca(2+) stores and phosphorylation of eIF2alpha.
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