Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles
Autor(a) principal: | |
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Data de Publicação: | 2014 |
Outros Autores: | , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10316/27929 https://doi.org/10.1016/j.ejmech.2014.04.008 |
Resumo: | Further studies on 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles as anticancer agents against breast cancer are reported, allowing to demonstrate the potential of these compounds for the therapy of the triple-negative breast cancer, the most challenging tumors in clinical practice. These compounds were assayed for their in vitro cytotoxicity on several human breast cancer cell lines (MCF7, HCC1954 and HCC1806 cell lines). Particularly interesting were the results obtained for 4-hydroxyphenyl substituted derivative, which proved to be the most promising compound regarding HCC1806 cell line, a triple-negative breast cancer. The effects of the two most active compounds on cell survival, viability, cell cycle, DNA damage and expression of proteins related to cell death pathways were studied. The reported results consolidate the potential of 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles for the therapy of breast cancer, particularly the triple-negative. |
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Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles6,7-Bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoleAntitumor activityBreast cancerTriple-negative breast cancerFurther studies on 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles as anticancer agents against breast cancer are reported, allowing to demonstrate the potential of these compounds for the therapy of the triple-negative breast cancer, the most challenging tumors in clinical practice. These compounds were assayed for their in vitro cytotoxicity on several human breast cancer cell lines (MCF7, HCC1954 and HCC1806 cell lines). Particularly interesting were the results obtained for 4-hydroxyphenyl substituted derivative, which proved to be the most promising compound regarding HCC1806 cell line, a triple-negative breast cancer. The effects of the two most active compounds on cell survival, viability, cell cycle, DNA damage and expression of proteins related to cell death pathways were studied. The reported results consolidate the potential of 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles for the therapy of breast cancer, particularly the triple-negative.Elsevier2014-05-22info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/27929http://hdl.handle.net/10316/27929https://doi.org/10.1016/j.ejmech.2014.04.008engSANTOS, Kathleen [et. al] - Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles. "European Journal of Medicinal Chemistry". ISSN 0223-5234. Vol. 79 (2014) p. 273–2810223-5234http://www.sciencedirect.com/science/article/pii/S0223523414003274Santos, KathleenLaranjo, MafaldaAbrantes, Ana MargaridaBrito, Ana F.Gonçalves, CristinaRibeiro, Ana Bela SarmentoBotelho, M. FilomenaSoares, Maria I. L.Oliveira, Andreia S. R.Melo, Teresa M. V. D. Pinho einfo:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2020-05-29T10:05:10Zoai:estudogeral.uc.pt:10316/27929Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T20:43:40.942685Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles |
title |
Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles |
spellingShingle |
Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles Santos, Kathleen 6,7-Bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazole Antitumor activity Breast cancer Triple-negative breast cancer |
title_short |
Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles |
title_full |
Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles |
title_fullStr |
Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles |
title_full_unstemmed |
Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles |
title_sort |
Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles |
author |
Santos, Kathleen |
author_facet |
Santos, Kathleen Laranjo, Mafalda Abrantes, Ana Margarida Brito, Ana F. Gonçalves, Cristina Ribeiro, Ana Bela Sarmento Botelho, M. Filomena Soares, Maria I. L. Oliveira, Andreia S. R. Melo, Teresa M. V. D. Pinho e |
author_role |
author |
author2 |
Laranjo, Mafalda Abrantes, Ana Margarida Brito, Ana F. Gonçalves, Cristina Ribeiro, Ana Bela Sarmento Botelho, M. Filomena Soares, Maria I. L. Oliveira, Andreia S. R. Melo, Teresa M. V. D. Pinho e |
author2_role |
author author author author author author author author author |
dc.contributor.author.fl_str_mv |
Santos, Kathleen Laranjo, Mafalda Abrantes, Ana Margarida Brito, Ana F. Gonçalves, Cristina Ribeiro, Ana Bela Sarmento Botelho, M. Filomena Soares, Maria I. L. Oliveira, Andreia S. R. Melo, Teresa M. V. D. Pinho e |
dc.subject.por.fl_str_mv |
6,7-Bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazole Antitumor activity Breast cancer Triple-negative breast cancer |
topic |
6,7-Bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazole Antitumor activity Breast cancer Triple-negative breast cancer |
description |
Further studies on 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles as anticancer agents against breast cancer are reported, allowing to demonstrate the potential of these compounds for the therapy of the triple-negative breast cancer, the most challenging tumors in clinical practice. These compounds were assayed for their in vitro cytotoxicity on several human breast cancer cell lines (MCF7, HCC1954 and HCC1806 cell lines). Particularly interesting were the results obtained for 4-hydroxyphenyl substituted derivative, which proved to be the most promising compound regarding HCC1806 cell line, a triple-negative breast cancer. The effects of the two most active compounds on cell survival, viability, cell cycle, DNA damage and expression of proteins related to cell death pathways were studied. The reported results consolidate the potential of 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles for the therapy of breast cancer, particularly the triple-negative. |
publishDate |
2014 |
dc.date.none.fl_str_mv |
2014-05-22 |
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://hdl.handle.net/10316/27929 http://hdl.handle.net/10316/27929 https://doi.org/10.1016/j.ejmech.2014.04.008 |
url |
http://hdl.handle.net/10316/27929 https://doi.org/10.1016/j.ejmech.2014.04.008 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
SANTOS, Kathleen [et. al] - Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles. "European Journal of Medicinal Chemistry". ISSN 0223-5234. Vol. 79 (2014) p. 273–281 0223-5234 http://www.sciencedirect.com/science/article/pii/S0223523414003274 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.publisher.none.fl_str_mv |
Elsevier |
publisher.none.fl_str_mv |
Elsevier |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
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Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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RCAAP |
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RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
repository.name.fl_str_mv |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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1799133708604669952 |