| Author | Silva, Thiago David dos Santos | |
| Author | Bomfim, Larissa Mendes | |
| Author | Rodrigues, Ana Carolina Borges da Cruz | |
| Author | Dias, Rosane Borges | |
| Author | Sales, Caroline Brandi Schlaepfer | |
| Author | Rocha, Clarissa Araújo Gurgel | |
| Author | Soares, Milena Botelho Pereira | |
| Author | Bezerra, Daniel Pereira | |
| Author | Cardoso, Marcos Veríssimo de Oliveira | |
| Author | Leite, Ana Cristina Lima | |
| Author | Militão, Gardenia Carmen Gadelha | |
| Access date | 2017-07-17T16:45:29Z | |
| Available date | 2017-07-17T16:45:29Z | |
| Document date | 2017 | |
| 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. | pt_BR |
| ISSN | 0041-008X | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/20109 | |
| Sponsorship | CAPES, CNPq, FAPESB and FACEPE. (APQ-0213-2.10/13; AMD-0050-4.03/16) | pt_BR |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | open access | pt_BR |
| Subject in Portuguese | HepG2 | pt_BR |
| Subject in Portuguese | Antitumor | pt_BR |
| Subject in Portuguese | Citotoxicidade | pt_BR |
| Subject in Portuguese | Câncer de fígado | pt_BR |
| Subject in Portuguese | Toxicidade | pt_BR |
| Title | Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives | pt_BR |
| Type | Article | pt_BR |
| DOI | 10.1016/j.taap.2017.06.003 | |
| 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. | pt_BR |
| 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 | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
| Affilliation | Federal University of Bahia. Institute of Health Sciences. Department of Biomorphology. Salvador, BA, Brazil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Center of Biotechnology and Cell therapy. Salvador, BA, Brazil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
| Affilliation | University of Pernambuco. Collegiate of Nutrition. Petrolina, PE, Brazil | pt_BR |
| Affilliation | Federal University of Pernambuco. Health Sciences Center. Department of Pharmaceutical Sciences. Recife, PE, Brazil | pt_BR |
| Affilliation | Federal University of Pernambuco. Department of Physiology and Pharmacology. Recife, PE, Brazil | pt_BR |
| Subject | HepG2 | pt_BR |
| Subject | Antitumor | pt_BR |
| Subject | Cytotoxicity | pt_BR |
| Subject | Cancer Liver | pt_BR |
| Subject | Toxicity | pt_BR |
