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ID: ALA3120078

Journal: Eur J Med Chem

Title: Benzofuran derivatives as a novel class of inhibitors of mTOR signaling.

Authors: Salomé C, Narbonne V, Ribeiro N, Thuaud F, Serova M, de Gramont A, Faivre S, Raymond E, Désaubry L.

Abstract: High-throughput screening (HTS) hit 1 was previously identified as an inhibitor of the Akt/mTOR (Akt/mammalian target of rapamycin) signaling, which is a major target in oncology. The cytotoxicity of 1 was determined on a panel of human cancer cells lines with an IC₅₀ comprised between 30 and 140 μM. Subsequent structure--activity relationship (SAR) studies led us to the identification of compounds that displayed an enhanced cytotoxicity. We demonstrated also that these molecules directly bind to mTOR complex 1 (mTORC1) and inhibit its kinase activity.

CiteXplore: 24445311

DOI: 10.1016/j.ejmech.2013.12.020