Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives

• Autor(a) principal: Silva, Thiago David dos Santos
• Data de Publicação: 2018
• Outros Autores: 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
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Institucional da UFBA
• Texto Completo: http://repositorio.ufba.br/ri/handle/ri/25931
• topic: 2-Pyridyl 2,3-thiazoles; HepG2; Cytotoxicity; Antitumor; Liver Cancer; Toxicity

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.