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Please use this identifier to cite or link to this item: http://repositorio.ufba.br/ri/handle/ri/25931

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
Keywords: 2-Pyridyl 2,3-thiazoles;HepG2;Cytotoxicity;Antitumor;Liver Cancer;Toxicity
Issue Date: 4-May-2018
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 ≤ 3 μM), 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 5.6 μM, respectively) without antiproliferative effects to normal cells (PBMC) (IC50 N 30 μM),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 immunodeficientmice. Systemic toxicological verified by biochemical and histopathological techniques reveled nomajor signs of toxicity after treatmentwith TAP-07 and TP-07. Together the results indicated the anti-liver cancer activity of 2-pyridyl 2,3-thiazole derivatives.
URI: http://repositorio.ufba.br/ri/handle/ri/25931
ISSN: (0041-008X) Toxicology and Applied Pharmacology
Appears in Collections:Artigos Publicados em Periódicos (Renorbio)

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