Please use this identifier to cite or link to this item: http://www.arca.fiocruz.br/handle/icict/20109
Title: Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives
Authors: Silva, Thiago David dos Santos
Bomfim, Larissa Mendes
Rodrigues, Ana Carolina Borges da Cruz
Dias, Rosane Borges
Sales, Caroline Brandi Schlaepfer
Rocha, Clarissa Araújo Gurgel
Soares, Milena Botelho Pereira
Bezerra, Daniel Pereira
Cardoso, Marcos Veríssimo de Oliveira
Leite, Ana Cristina Lima
Militão, Gardenia Carmen Gadelha
Affilliation: Federal University of Pernambuco. Health Sciences Center. Department of Pharmaceutical Sciences. Recife, PE, Brazil / Federal University of Pernambuco. Department of Physiology and Pharmacology. Recife, PE, Brazil
Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil
Federal University of Bahia. Institute of Health Sciences. Department of Biomorphology. Salvador, BA, Brazil
Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Center of Biotechnology and Cell therapy. Salvador, BA, Brazil
Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil
University of Pernambuco. Collegiate of Nutrition. Petrolina, PE, Brazil
Federal University of Pernambuco. Health Sciences Center. Department of Pharmaceutical Sciences. Recife, PE, Brazil
Federal University of Pernambuco. Department of Physiology and Pharmacology. Recife, PE, Brazil
Abstract: A total of 24 hybrid compounds containing pyridyl and 1,3-thiazole moieties were screened against HL-60 (leukemia), MCF-7 (breast adenocarcinoma), HepG2 (hepatocellular carcinoma), NCI-H292 (lung carcinoma) human tumor cell lines and non-tumor cells (PBMC, human peripheral blood mononuclear cells). Most of them were highly potent in at least one cell line tested (IC50≤3μM), being HL-60 the most sensitive and HepG2 the most resistant cell line. Among them, TAP-07 and TP-07 presented cytotoxic activity in all tumor cell lines, including HepG2 (IC50 2.2 and 5.6μM, respectively) without antiproliferative effects to normal cells (PBMC) (IC50>30μM), making TAP-07 and TP-07, the compounds with the most favorable selectivity index. TAP-07 and TP-07 induced apoptosis in HepG2 cells and presented in vivo antitumor activity in hepatocellular xenograft cancer model in C.B-17 severe combined immunodeficient mice. Systemic toxicological verified by biochemical and histopathological techniques reveled no major signs of toxicity after treatment with TAP-07 and TP-07. Together the results indicated the anti-liver cancer activity of 2-pyridyl 2,3-thiazole derivatives.
Keywords: 2-Pyridyl 2,3-thiazoles
HepG2
Antitumor
Cytotoxicity
Cancer Liver
Toxicity
keywords: 2-piridil 2,3-tiazoles
HepG2
Antitumor
Citotoxicidade
Câncer de fígado
Toxicidade
Issue Date: 2017
Publisher: Elsevier
Citation: SILVA, T. D. S. et al. Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives. Toxicology and Applied Pharmacology, v. 329, p. 212–223, 2017.
DOI: 10.1016/j.taap.2017.06.003
ISSN: 0041-008X
Copyright: open access
Appears in Collections:IGM - Artigos de Periódicos

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