Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80)

Detalhes bibliográficos
Autor(a) principal: Aleixo,Mariana A. A.
Data de Publicação: 2018
Outros Autores: 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.
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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spelling 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

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