Santos, Mariana B. [UNESP]Pinhanelli, Vitor C.Garcia, Mayara A.R. [UNESP]Silva, GabrielBaek, Seung J.França, Suzelei C.Fachin, Ana L.Marins, MozartRegasini, Luis O. [UNESP]2018-12-112018-12-112017-01-01European Journal of Medicinal Chemistry, v. 138, p. 884-889.1768-32540223-5234http://hdl.handle.net/11449/174929In the present study, a series of 2′- and 4′-aminochalcones were synthesized and their antiproliferative activity against a canine malignant histiocytic cell line (DH82) was evaluated. Particularly aminochalcones with a hydrophobic substituent on ring B proved to be potent antiproliferative agents. Among these compounds, aminochalcones 3, 4 and 11 inhibited the growth of DH82 cells, with IC50 values of 34.4, 31.4 and 38.2 μM, respectively, and were three times more potent than etoposide (IC50 = 95.5 μM). The selected chalcones induced death through apoptosis rather than necrosis in DH82 and non-tumorigenic Madin-Darby canine kidney cells (MDCK). Further experiments suggested that the aminochalcones interfere with the regulation of oncogenes/tumor suppressor genes. Aminochalcone 11 inhibited transcription of the TOPOIIα and TP53 genes and aminochalcone 4 down-regulated Sp1 protein expression in a concentration-dependent manner.884-889engAntiproliferativeApoptosisCanine cancerChalconeArtigo10.1016/j.ejmech.2017.06.049Acesso aberto2-s2.0-850248848652-s2.0-85024884865.pdf