Anti-proliferative effects of novel hydroxyamides and triazoles
Autor(a) principal: | |
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Data de Publicação: | 2016 |
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/10174/20090 https://doi.org/10.1016/j.nbt.2015.10.008 |
Resumo: | Chemotherapy is a major cancer treatment option. The synthesis of new compounds with anti-proliferative properties and specificity is a current challenge in drug-discovery today. Our goal was to develop compounds, either hydroxyamides derived from D-glucuronic acid or triazole-cinchone hybrids, and to evaluate their anti-proliferative properties. Anti-proliferative activity of the newly synthesized compounds was examined against human breast adenocarcinoma (MCF-7) and human colon carcinoma (MDST8) cell-lines. Cell growth and viability was analysed by the Cell-Counting Kit-8 method. The 5-fluoroacil was used as a positive control. The compounds were studied between 10-9-10-5M. Fifteen compounds from the hydroxyamide family and two triazole compounds were investigated. Most of the compounds from the hydroxyamide family revealed mild (~20%) to moderate (50%) anti-proliferative effects in both cell-lines, with the exception of Hydroxyamide B1 which did not affect MDST8 proliferation, and hydroxyamide B3 where proliferation of MDST8 was inhibited by 90%. Triazoles (A and B) evoked a strong (~100%) anti-proliferative effect of MDST8 cell-lines. Proliferation of MCF-7 was selectively and effectively (~98%) inhibited by triazole B while triazole A had a mild effect. In conclusion, when compared to hydroxyamides, triazoles evoked a stronger anti-proliferative effect and might be promising anti-tumoral drugs. |
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Anti-proliferative effects of novel hydroxyamides and triazolesanti-proliferativehydroxyamidestriazolesChemotherapy is a major cancer treatment option. The synthesis of new compounds with anti-proliferative properties and specificity is a current challenge in drug-discovery today. Our goal was to develop compounds, either hydroxyamides derived from D-glucuronic acid or triazole-cinchone hybrids, and to evaluate their anti-proliferative properties. Anti-proliferative activity of the newly synthesized compounds was examined against human breast adenocarcinoma (MCF-7) and human colon carcinoma (MDST8) cell-lines. Cell growth and viability was analysed by the Cell-Counting Kit-8 method. The 5-fluoroacil was used as a positive control. The compounds were studied between 10-9-10-5M. Fifteen compounds from the hydroxyamide family and two triazole compounds were investigated. Most of the compounds from the hydroxyamide family revealed mild (~20%) to moderate (50%) anti-proliferative effects in both cell-lines, with the exception of Hydroxyamide B1 which did not affect MDST8 proliferation, and hydroxyamide B3 where proliferation of MDST8 was inhibited by 90%. Triazoles (A and B) evoked a strong (~100%) anti-proliferative effect of MDST8 cell-lines. Proliferation of MCF-7 was selectively and effectively (~98%) inhibited by triazole B while triazole A had a mild effect. In conclusion, when compared to hydroxyamides, triazoles evoked a stronger anti-proliferative effect and might be promising anti-tumoral drugs.Elsevier2017-01-27T10:42:47Z2017-01-272016-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10174/20090http://hdl.handle.net/10174/20090https://doi.org/10.1016/j.nbt.2015.10.008engTiago S. Martins, Tiago O. Pires, Maria M. Cordeiro, Rute Martins, Elisabete P. Carreiro, Luis Alves, Anthony Burke, Célia M. Antunes, Ana R. Costa (2016) "Anti-proliferative effects of novel hydroxyamides and triazoles", NEW BIOTECHNOLOGY 33(3), 416-417.http://www.sciencedirect.com/science/article/pii/S1871678415001776ICAAM; ICTndndndndbete_carreiro@yahoo.comndajb@uevora.ptcmma@uevora.ptacrc@uevora.pt365Martins, Tiago S.Pires, Tiago O.Cordeiro, Maria M.Martins, RuteCarreiro, ElisabeteAlves, LuísBurke, AnthonyAntunes, Célia M.Costa, Ana R.info: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:RCAAP2024-01-03T19:09:57Zoai:dspace.uevora.pt:10174/20090Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T01:11:45.080168Repositório 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 |
Anti-proliferative effects of novel hydroxyamides and triazoles |
title |
Anti-proliferative effects of novel hydroxyamides and triazoles |
spellingShingle |
Anti-proliferative effects of novel hydroxyamides and triazoles Martins, Tiago S. anti-proliferative hydroxyamides triazoles |
title_short |
Anti-proliferative effects of novel hydroxyamides and triazoles |
title_full |
Anti-proliferative effects of novel hydroxyamides and triazoles |
title_fullStr |
Anti-proliferative effects of novel hydroxyamides and triazoles |
title_full_unstemmed |
Anti-proliferative effects of novel hydroxyamides and triazoles |
title_sort |
Anti-proliferative effects of novel hydroxyamides and triazoles |
author |
Martins, Tiago S. |
author_facet |
Martins, Tiago S. Pires, Tiago O. Cordeiro, Maria M. Martins, Rute Carreiro, Elisabete Alves, Luís Burke, Anthony Antunes, Célia M. Costa, Ana R. |
author_role |
author |
author2 |
Pires, Tiago O. Cordeiro, Maria M. Martins, Rute Carreiro, Elisabete Alves, Luís Burke, Anthony Antunes, Célia M. Costa, Ana R. |
author2_role |
author author author author author author author author |
dc.contributor.author.fl_str_mv |
Martins, Tiago S. Pires, Tiago O. Cordeiro, Maria M. Martins, Rute Carreiro, Elisabete Alves, Luís Burke, Anthony Antunes, Célia M. Costa, Ana R. |
dc.subject.por.fl_str_mv |
anti-proliferative hydroxyamides triazoles |
topic |
anti-proliferative hydroxyamides triazoles |
description |
Chemotherapy is a major cancer treatment option. The synthesis of new compounds with anti-proliferative properties and specificity is a current challenge in drug-discovery today. Our goal was to develop compounds, either hydroxyamides derived from D-glucuronic acid or triazole-cinchone hybrids, and to evaluate their anti-proliferative properties. Anti-proliferative activity of the newly synthesized compounds was examined against human breast adenocarcinoma (MCF-7) and human colon carcinoma (MDST8) cell-lines. Cell growth and viability was analysed by the Cell-Counting Kit-8 method. The 5-fluoroacil was used as a positive control. The compounds were studied between 10-9-10-5M. Fifteen compounds from the hydroxyamide family and two triazole compounds were investigated. Most of the compounds from the hydroxyamide family revealed mild (~20%) to moderate (50%) anti-proliferative effects in both cell-lines, with the exception of Hydroxyamide B1 which did not affect MDST8 proliferation, and hydroxyamide B3 where proliferation of MDST8 was inhibited by 90%. Triazoles (A and B) evoked a strong (~100%) anti-proliferative effect of MDST8 cell-lines. Proliferation of MCF-7 was selectively and effectively (~98%) inhibited by triazole B while triazole A had a mild effect. In conclusion, when compared to hydroxyamides, triazoles evoked a stronger anti-proliferative effect and might be promising anti-tumoral drugs. |
publishDate |
2016 |
dc.date.none.fl_str_mv |
2016-01-01T00:00:00Z 2017-01-27T10:42:47Z 2017-01-27 |
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/10174/20090 http://hdl.handle.net/10174/20090 https://doi.org/10.1016/j.nbt.2015.10.008 |
url |
http://hdl.handle.net/10174/20090 https://doi.org/10.1016/j.nbt.2015.10.008 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Tiago S. Martins, Tiago O. Pires, Maria M. Cordeiro, Rute Martins, Elisabete P. Carreiro, Luis Alves, Anthony Burke, Célia M. Antunes, Ana R. Costa (2016) "Anti-proliferative effects of novel hydroxyamides and triazoles", NEW BIOTECHNOLOGY 33(3), 416-417. http://www.sciencedirect.com/science/article/pii/S1871678415001776 ICAAM; ICT nd nd nd nd bete_carreiro@yahoo.com nd ajb@uevora.pt cmma@uevora.pt acrc@uevora.pt 365 |
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 |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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1799136599407067136 |