Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives
Autor(a) principal: | |
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Data de Publicação: | 2018 |
Outros Autores: | , , , , , , , , , |
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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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). 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)10.1016/j.taap.2017.06.003reponame:Repositório Institucional da UFBAinstname:Universidade Federal da Bahia (UFBA)instacron:UFBA2-Pyridyl 2,3-thiazolesHepG2CytotoxicityAntitumorLiver CancerToxicityAnti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivativesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleBrasilinfo:eu-repo/semantics/openAccessengORIGINALANTI-LIVER CANCER ACTIVITY IN VITRO AND IN VIVO INDUCED BY 2-PYRIDYL 2,3-THIAZOLE DERIVATIVES.pdfANTI-LIVER CANCER ACTIVITY IN VITRO AND IN VIVO INDUCED BY 2-PYRIDYL 2,3-THIAZOLE DERIVATIVES.pdfapplication/pdf2793458https://repositorio.ufba.br/bitstream/ri/25931/1/ANTI-LIVER%20CANCER%20ACTIVITY%20IN%20VITRO%20AND%20IN%20VIVO%20INDUCED%20BY%202-PYRIDYL%202%2c3-THIAZOLE%20DERIVATIVES.pdffcbb9a4336522af9d68dd7cdd4ded487MD51LICENSElicense.txtlicense.txttext/plain1383https://repositorio.ufba.br/bitstream/ri/25931/2/license.txt05eca2f01d0b3307819d0369dab18a34MD52TEXTANTI-LIVER CANCER ACTIVITY IN VITRO AND IN VIVO INDUCED BY 2-PYRIDYL 2,3-THIAZOLE DERIVATIVES.pdf.txtANTI-LIVER CANCER ACTIVITY IN VITRO AND IN VIVO INDUCED BY 2-PYRIDYL 2,3-THIAZOLE DERIVATIVES.pdf.txtExtracted texttext/plain51376https://repositorio.ufba.br/bitstream/ri/25931/3/ANTI-LIVER%20CANCER%20ACTIVITY%20IN%20VITRO%20AND%20IN%20VIVO%20INDUCED%20BY%202-PYRIDYL%202%2c3-THIAZOLE%20DERIVATIVES.pdf.txt19683714973f1fb39ee91d4f898e9a75MD53ri/259312022-07-05 14:03:49.13oai:repositorio.ufba.br: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ório InstitucionalPUBhttp://192.188.11.11:8080/oai/requestopendoar:19322022-07-05T17:03:49Repositório Institucional da UFBA - Universidade Federal da Bahia (UFBA)false |
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 |
format |
article |
status_str |
publishedVersion |
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 instname:Universidade Federal da Bahia (UFBA) instacron:UFBA |
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Universidade Federal da Bahia (UFBA) |
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UFBA |
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UFBA |
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Repositório Institucional da UFBA |
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Repositório Institucional da UFBA |
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