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

Detalhes bibliográficos
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
Resumo: 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.
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spelling Silva, Thiago David dos SantosBomfim, Larissa MendesRodrigues, Ana Carolina Borges da CruzDias, Rosane BorgesSales, Caroline Brandi SchlaepferRocha, Clarissa Araújo GurgelSoares, Milena Botelho PereiraBezerra, Daniel PereiraCardoso, Marcos Veríssimo de OliveiraLeite, Ana Cristina LimaMilitão, Gardenia Carmen GadelhaSilva, Thiago David dos SantosBomfim, Larissa MendesRodrigues, Ana Carolina Borges da CruzDias, Rosane BorgesSales, Caroline Brandi SchlaepferRocha, Clarissa Araújo GurgelSoares, Milena Botelho PereiraBezerra, Daniel PereiraCardoso, Marcos Veríssimo de OliveiraLeite, Ana Cristina LimaMilitão, Gardenia Carmen Gadelha2018-05-04T14:23:31Z2018-05-04T14:23:31Z2018-05-04(0041-008X) Toxicology and Applied Pharmacologyhttp://repositorio.ufba.br/ri/handle/ri/25931329A 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.Submitted by Renorbio (renorbioba@ufba.br) on 2018-05-02T18:48:24Z No. of bitstreams: 1 ANTI-LIVER CANCER ACTIVITY IN VITRO AND IN VIVO INDUCED BY 2-PYRIDYL 2,3-THIAZOLE DERIVATIVES.pdf: 2793458 bytes, checksum: fcbb9a4336522af9d68dd7cdd4ded487 (MD5)Approved for entry into archive by Delba Rosa (delba@ufba.br) on 2018-05-04T14:23:31Z (GMT) No. of bitstreams: 1 ANTI-LIVER CANCER ACTIVITY IN VITRO AND IN VIVO INDUCED BY 2-PYRIDYL 2,3-THIAZOLE DERIVATIVES.pdf: 2793458 bytes, checksum: fcbb9a4336522af9d68dd7cdd4ded487 (MD5)Made available in DSpace on 2018-05-04T14:23:31Z (GMT). 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dc.title.pt_BR.fl_str_mv Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives
title Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives
spellingShingle Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives
Silva, Thiago David dos Santos
2-Pyridyl 2,3-thiazoles
HepG2
Cytotoxicity
Antitumor
Liver Cancer
Toxicity
title_short Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives
title_full Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives
title_fullStr Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives
title_full_unstemmed Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives
title_sort Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives
author Silva, Thiago David dos Santos
author_facet 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
author_role author
author2 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
author2_role author
author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv 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
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
dc.subject.por.fl_str_mv 2-Pyridyl 2,3-thiazoles
HepG2
Cytotoxicity
Antitumor
Liver Cancer
Toxicity
topic 2-Pyridyl 2,3-thiazoles
HepG2
Cytotoxicity
Antitumor
Liver Cancer
Toxicity
description 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.
publishDate 2018
dc.date.accessioned.fl_str_mv 2018-05-04T14:23:31Z
dc.date.available.fl_str_mv 2018-05-04T14:23:31Z
dc.date.issued.fl_str_mv 2018-05-04
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
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dc.identifier.uri.fl_str_mv http://repositorio.ufba.br/ri/handle/ri/25931
dc.identifier.issn.none.fl_str_mv (0041-008X) Toxicology and Applied Pharmacology
dc.identifier.number.pt_BR.fl_str_mv 329
identifier_str_mv (0041-008X) Toxicology and Applied Pharmacology
329
url http://repositorio.ufba.br/ri/handle/ri/25931
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.country.fl_str_mv Brasil
dc.source.pt_BR.fl_str_mv 10.1016/j.taap.2017.06.003
dc.source.none.fl_str_mv reponame:Repositório Institucional da UFBA
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