Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80)
Autor(a) principal: | |
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Data de Publicação: | 2018 |
Outros Autores: | , , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Journal of the Brazilian Chemical Society (Online) |
Texto Completo: | http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532018000100109 |
Resumo: | We report herein the design and synthesis via click chemistry of twelve novel triazole retinoid analogues of tamibarotene (AM80) and the evaluation of their anticancer activities against six cancer cell lines: HL60, K562, 786, HT29, MCF7 and PC3. Among the synthesized compounds, two were more potent than tamibarotene against solid tumor cells, and one of them had similar potency to tamibarotene against HL60 cells. The bioisosteric exchange between the amide group and the 1,2,3-triazole core in the retinoid agent tamibarotene (AM80) reported in this work is a valid strategy for the generation of useful compounds against cancer. |
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Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80)1,2,3-triazole retinoidstamibaroteneclick chemistrybioisosterismanticancer activitiesWe report herein the design and synthesis via click chemistry of twelve novel triazole retinoid analogues of tamibarotene (AM80) and the evaluation of their anticancer activities against six cancer cell lines: HL60, K562, 786, HT29, MCF7 and PC3. Among the synthesized compounds, two were more potent than tamibarotene against solid tumor cells, and one of them had similar potency to tamibarotene against HL60 cells. The bioisosteric exchange between the amide group and the 1,2,3-triazole core in the retinoid agent tamibarotene (AM80) reported in this work is a valid strategy for the generation of useful compounds against cancer.Sociedade Brasileira de Química2018-01-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532018000100109Journal of the Brazilian Chemical Society v.29 n.1 2018reponame:Journal of the Brazilian Chemical Society (Online)instname:Sociedade Brasileira de Química (SBQ)instacron:SBQ10.21577/0103-5053.20170119info:eu-repo/semantics/openAccessAleixo,Mariana A. A.Garcia,Taís M.Carvalho,Diego B.Viana,Luiz H.Amaral,Marcos S.Kassab,Najla M.Cunha,Marilin C.Pereira,Indiara C.Guerrero Jr.,Palimécio G.Perdomo,Renata T.Matos,Maria F. C.Baroni,Adriano C. M.eng2018-02-08T00:00:00Zoai:scielo:S0103-50532018000100109Revistahttp://jbcs.sbq.org.brONGhttps://old.scielo.br/oai/scielo-oai.php||office@jbcs.sbq.org.br1678-47900103-5053opendoar:2018-02-08T00:00Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)false |
dc.title.none.fl_str_mv |
Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80) |
title |
Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80) |
spellingShingle |
Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80) Aleixo,Mariana A. A. 1,2,3-triazole retinoids tamibarotene click chemistry bioisosterism anticancer activities |
title_short |
Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80) |
title_full |
Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80) |
title_fullStr |
Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80) |
title_full_unstemmed |
Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80) |
title_sort |
Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80) |
author |
Aleixo,Mariana A. A. |
author_facet |
Aleixo,Mariana A. A. Garcia,Taís M. Carvalho,Diego B. Viana,Luiz H. Amaral,Marcos S. Kassab,Najla M. Cunha,Marilin C. Pereira,Indiara C. Guerrero Jr.,Palimécio G. Perdomo,Renata T. Matos,Maria F. C. Baroni,Adriano C. M. |
author_role |
author |
author2 |
Garcia,Taís M. Carvalho,Diego B. Viana,Luiz H. Amaral,Marcos S. Kassab,Najla M. Cunha,Marilin C. Pereira,Indiara C. Guerrero Jr.,Palimécio G. Perdomo,Renata T. Matos,Maria F. C. Baroni,Adriano C. M. |
author2_role |
author author author author author author author author author author author |
dc.contributor.author.fl_str_mv |
Aleixo,Mariana A. A. Garcia,Taís M. Carvalho,Diego B. Viana,Luiz H. Amaral,Marcos S. Kassab,Najla M. Cunha,Marilin C. Pereira,Indiara C. Guerrero Jr.,Palimécio G. Perdomo,Renata T. Matos,Maria F. C. Baroni,Adriano C. M. |
dc.subject.por.fl_str_mv |
1,2,3-triazole retinoids tamibarotene click chemistry bioisosterism anticancer activities |
topic |
1,2,3-triazole retinoids tamibarotene click chemistry bioisosterism anticancer activities |
description |
We report herein the design and synthesis via click chemistry of twelve novel triazole retinoid analogues of tamibarotene (AM80) and the evaluation of their anticancer activities against six cancer cell lines: HL60, K562, 786, HT29, MCF7 and PC3. Among the synthesized compounds, two were more potent than tamibarotene against solid tumor cells, and one of them had similar potency to tamibarotene against HL60 cells. The bioisosteric exchange between the amide group and the 1,2,3-triazole core in the retinoid agent tamibarotene (AM80) reported in this work is a valid strategy for the generation of useful compounds against cancer. |
publishDate |
2018 |
dc.date.none.fl_str_mv |
2018-01-01 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532018000100109 |
url |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532018000100109 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
10.21577/0103-5053.20170119 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
text/html |
dc.publisher.none.fl_str_mv |
Sociedade Brasileira de Química |
publisher.none.fl_str_mv |
Sociedade Brasileira de Química |
dc.source.none.fl_str_mv |
Journal of the Brazilian Chemical Society v.29 n.1 2018 reponame:Journal of the Brazilian Chemical Society (Online) instname:Sociedade Brasileira de Química (SBQ) instacron:SBQ |
instname_str |
Sociedade Brasileira de Química (SBQ) |
instacron_str |
SBQ |
institution |
SBQ |
reponame_str |
Journal of the Brazilian Chemical Society (Online) |
collection |
Journal of the Brazilian Chemical Society (Online) |
repository.name.fl_str_mv |
Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ) |
repository.mail.fl_str_mv |
||office@jbcs.sbq.org.br |
_version_ |
1750318180369170432 |