Author(s): Santos, Mariana B. [UNESP] ; Pinhanelli, Vitor C. ; Garcia, Mayara A.R. [UNESP] ; Silva, Gabriel ; Baek, Seung J. ; França, Suzelei C. ; Fachin, Ana L. ; Marins, Mozart ; Regasini, Luis O. [UNESP]
Date: 2018
Persistent ID: http://hdl.handle.net/11449/174929
Origin: Oasisbr
Subject(s): Antiproliferative; Apoptosis; Canine cancer; Chalcone
Made available in DSpace on 2018-12-11T17:13:30Z (GMT). No. of bitstreams: 0 Previous issue date: 2017-01-01
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
In 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.
Department of Chemistry and Environmental Sciences Institute of Biosciences Humanities and Exact Sciences (Ibilce) São Paulo State University (Unesp), Campus São José do Rio Preto
Biotechnology Unit University of Ribeirão Preto
Department of Biomedical and Diagnostic Sciences College of Veterinary Medicine University of Tennessee
School of Medicine University of Ribeirão Preto
Department of Chemistry and Environmental Sciences Institute of Biosciences Humanities and Exact Sciences (Ibilce) São Paulo State University (Unesp), Campus São José do Rio Preto
FAPESP: 2014/15307-7
FAPESP: 2014/18330-0
CNPq: 306251/2016-7
CNPq: 471129/2013-5
