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Antiproliferative and pro-apoptotic activities of 2'- and 4'-aminochalcones against tumor canine cells.
Santos, Mariana B; Pinhanelli, Vitor C; Garcia, Mayara A R; Silva, Gabriel; Baek, Seung J; França, Suzelei C; Fachin, Ana L; Marins, Mozart; Regasini, Luis O.
Afiliação
  • Santos MB; 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, SP, Brazil.
  • Pinhanelli VC; Biotechnology Unit, University of Ribeirão Preto, Ribeirão Preto, SP, Brazil.
  • Garcia MAR; 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, SP, Brazil.
  • Silva G; Biotechnology Unit, University of Ribeirão Preto, Ribeirão Preto, SP, Brazil; Department of Biomedical and Diagnostic Sciences, College of Veterinary Medicine, University of Tennessee, Knoxville, TN, USA.
  • Baek SJ; Department of Biomedical and Diagnostic Sciences, College of Veterinary Medicine, University of Tennessee, Knoxville, TN, USA.
  • França SC; Biotechnology Unit, University of Ribeirão Preto, Ribeirão Preto, SP, Brazil.
  • Fachin AL; Biotechnology Unit, University of Ribeirão Preto, Ribeirão Preto, SP, Brazil; School of Medicine, University of Ribeirão Preto, Ribeirão Preto, SP, Brazil.
  • Marins M; Biotechnology Unit, University of Ribeirão Preto, Ribeirão Preto, SP, Brazil; School of Medicine, University of Ribeirão Preto, Ribeirão Preto, SP, Brazil. Electronic address: mmarins@gmb.bio.br.
  • Regasini LO; 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, SP, Brazil. Electronic address: regasini@ibilce.unesp.br.
Eur J Med Chem ; 138: 884-889, 2017 Sep 29.
Article em En | MEDLINE | ID: mdl-28738308
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Apoptose / Chalconas / Células Madin Darby de Rim Canino / Antineoplásicos Limite: Animals Idioma: En Revista: Eur J Med Chem Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Brasil País de publicação: França
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Apoptose / Chalconas / Células Madin Darby de Rim Canino / Antineoplásicos Limite: Animals Idioma: En Revista: Eur J Med Chem Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Brasil País de publicação: França