Abstract
Twenty-two hydroxyethylamine derivatives ((2S,3R)-2-(Amino)-[4-(N-benzylarenesulfonamido)-3-hydroxy-1-phenylbutane derivatives) containing aromatic sulfonamides were evaluated for their cytotoxic potential against three cancer cell lines using MTT assay. All compounds containing the Boc group, with the exception of 4i, were inactive at 5 μg/mL against all cell lines tested. Compounds 5c–e and 5g–i, containing the free amino group, displayed more than 95 % of growth inhibition (GI) and were selected for in vitro evaluation against peripheral blood mononuclear cells (PBMC) and four human cancer cell lines (HCT-116, OVCAR-8, HL-60, and SF-295). Tested compounds showed good cytotoxic activity against all cell lines (0.91–3.944 μg/mL). In general, the presence of electron withdrawing groups on the sulfonamide ring plays an important role in the anticancer activity of this series. It can also be pointed out that the free amino group in the hydroxyethylamine moiety is important for antitumoral activity since compounds 4a–j, containing a Boc group, were inactive. These results suggest the potential of hydroxyethylamine derivatives as lead compounds in anticancer drug discovery.
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The authors are grateful to the Brazilian agencies Capes (Coordenadoria de Apoio à Pesquisa e Ensino Superior), CNPq (Conselho Nacional de Desenvolvimento Cientifico e Tecnológico), FUNCAP-Ceará (Fundação de Pesquisa e Cultura) for fellowships and financial support and BiotechCell® Ltda.
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Facchinetti, V., Moreth, M., Gomes, C.R.B. et al. Evaluation of (2S,3R)-2-(amino)-[4-(N-benzylarenesulfonamido)-3-hydroxy-1-phenylbutane derivatives: a promising class of anticancer agents. Med Chem Res 24, 533–542 (2015). https://doi.org/10.1007/s00044-014-1143-5
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DOI: https://doi.org/10.1007/s00044-014-1143-5