Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines

Detalhes bibliográficos
Autor(a) principal: Aguiar, Andreza Conception Véras de
Data de Publicação: 2016
Outros Autores: Moura, Ricardo Olímpio de, Mendonça Junior, Jaime Francisco Bezerra, Rocha, Hugo Alexandre de Oliveira, Câmara, Rafael Barros Gomes da, Schiavon, Manuela dos Santos Carvalho
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UFRN
Texto Completo: https://repositorio.ufrn.br/handle/123456789/31316
Resumo: In spite of great progress in understanding cancer biology, current therapeutic procedures remain unsatisfactory. Chemotherapy is often followed by secondary effects with cellular toxicity negatively affecting the results. The discovery and development of new safe and efficient antitumor agents is necessary. Derivatives of 2-amino thiophene have been a topic of constant investigation due to their versatile synthetic applicability and broad spectrum of biological applications; among which are antifungal and antiproliferative activity shown in prior studies of our group. In the current study, compounds 6CN09, 6CN10, 6CN12, 6CN14, 7CN09 and 7CN11 were analyzed as to antiproliferative effect in human cells of cervical adenocarcinoma (HeLa), human pancreatic adenocarcinoma (PANC-1) and mice fibroblasts (3T3), which were exposed to the compounds in concentrations of 5, 10, 25 and 50mM during 24 and 48 h. They were submitted to MTT assay. In order to elucidate the action mechanism of antitumor thiophene derivatives flow cytometry was performed to evaluate cell death and cell cycle analysis. The results showed that thiophene derivatives demonstrated great antiproliferative potential in the HeLa and PANC-1 cell lines when compared with the control, and the percentage of cell proliferation inhibition approximated or was higher than the standard drug used; doxorubicin (Dox). In highlight were the derivatives 6CN14 and 7CN09 that showed greater efficiency in the antiproliferative evaluation. Further, all compounds had a protective effect on the non-tumor 3T3 cell line. The flow cytometry analysis showed few cells in apoptosis in both the HeLa and PANC-1 lines, although the compounds interfered with the progression of the cell cycle, and avoided cell growth and multiplication in the HeLa tumor line. These thiophene derivatives demonstrated cytostatic and antiproliferative effects and may be considered as promising molecular candidates for anticancer drugs
id UFRN_0d35920200c3bc43648a1086bec9385a
oai_identifier_str oai:https://repositorio.ufrn.br:123456789/31316
network_acronym_str UFRN
network_name_str Repositório Institucional da UFRN
repository_id_str
spelling Aguiar, Andreza Conception Véras deMoura, Ricardo Olímpio deMendonça Junior, Jaime Francisco BezerraRocha, Hugo Alexandre de OliveiraCâmara, Rafael Barros Gomes daSchiavon, Manuela dos Santos Carvalho2021-01-28T19:41:49Z2021-01-28T19:41:49Z2016-12AGUIAR, Andreza Conception Véras de; MOURA, Ricardo Olímpio de; MENDONÇA, Jaime Francisco Bezerra; ROCHA, Hugo Alexandre de Oliveira; CÂMARA, Rafael Barros Gomes da; SCHIAVON, Manuela dos Santos Carvalho. Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines. Biomedicine & Pharmacotherapy, [s. l.], v. 84, p. 403-414, dez. 2016. Elsevier BV. Disponível em: https://www.sciencedirect.com/science/article/abs/pii/S0753332216312185?via%3Dihub. Acesso em: 04 ago. 2020. Http://dx.doi.org/10.1016/j.biopha.2016.09.026.0753-3322 (print)https://repositorio.ufrn.br/handle/123456789/3131610.1016/j.biopha.2016.09.026ElsevierAnticancerAntiproliferativeCytostaticThiophene derivativesEvaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells linesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleIn spite of great progress in understanding cancer biology, current therapeutic procedures remain unsatisfactory. Chemotherapy is often followed by secondary effects with cellular toxicity negatively affecting the results. The discovery and development of new safe and efficient antitumor agents is necessary. Derivatives of 2-amino thiophene have been a topic of constant investigation due to their versatile synthetic applicability and broad spectrum of biological applications; among which are antifungal and antiproliferative activity shown in prior studies of our group. In the current study, compounds 6CN09, 6CN10, 6CN12, 6CN14, 7CN09 and 7CN11 were analyzed as to antiproliferative effect in human cells of cervical adenocarcinoma (HeLa), human pancreatic adenocarcinoma (PANC-1) and mice fibroblasts (3T3), which were exposed to the compounds in concentrations of 5, 10, 25 and 50mM during 24 and 48 h. They were submitted to MTT assay. In order to elucidate the action mechanism of antitumor thiophene derivatives flow cytometry was performed to evaluate cell death and cell cycle analysis. The results showed that thiophene derivatives demonstrated great antiproliferative potential in the HeLa and PANC-1 cell lines when compared with the control, and the percentage of cell proliferation inhibition approximated or was higher than the standard drug used; doxorubicin (Dox). In highlight were the derivatives 6CN14 and 7CN09 that showed greater efficiency in the antiproliferative evaluation. Further, all compounds had a protective effect on the non-tumor 3T3 cell line. The flow cytometry analysis showed few cells in apoptosis in both the HeLa and PANC-1 lines, although the compounds interfered with the progression of the cell cycle, and avoided cell growth and multiplication in the HeLa tumor line. These thiophene derivatives demonstrated cytostatic and antiproliferative effects and may be considered as promising molecular candidates for anticancer drugsengreponame:Repositório Institucional da UFRNinstname:Universidade Federal do Rio Grande do Norte (UFRN)instacron:UFRNinfo:eu-repo/semantics/openAccessCC-LICENSElicense_rdflicense_rdfapplication/rdf+xml; charset=utf-8914https://repositorio.ufrn.br/bitstream/123456789/31316/2/license_rdf4d2950bda3d176f570a9f8b328dfbbefMD52LICENSElicense.txtlicense.txttext/plain; charset=utf-81484https://repositorio.ufrn.br/bitstream/123456789/31316/3/license.txte9597aa2854d128fd968be5edc8a28d9MD53TEXTEvaluationAntiproliferativeActivity_Câmara_2016.pdf.txtEvaluationAntiproliferativeActivity_Câmara_2016.pdf.txtExtracted texttext/plain47749https://repositorio.ufrn.br/bitstream/123456789/31316/4/EvaluationAntiproliferativeActivity_C%c3%a2mara_2016.pdf.txtdcf22f16d2e8855dc69f6e2886d7bfdfMD54THUMBNAILEvaluationAntiproliferativeActivity_Câmara_2016.pdf.jpgEvaluationAntiproliferativeActivity_Câmara_2016.pdf.jpgGenerated Thumbnailimage/jpeg1719https://repositorio.ufrn.br/bitstream/123456789/31316/5/EvaluationAntiproliferativeActivity_C%c3%a2mara_2016.pdf.jpg033641a909af205a587448567709cbe9MD55123456789/313162023-01-26 15:18:35.831oai:https://repositorio.ufrn.br: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Repositório de PublicaçõesPUBhttp://repositorio.ufrn.br/oai/opendoar:2023-01-26T18:18:35Repositório Institucional da UFRN - Universidade Federal do Rio Grande do Norte (UFRN)false
dc.title.pt_BR.fl_str_mv Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines
title Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines
spellingShingle Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines
Aguiar, Andreza Conception Véras de
Anticancer
Antiproliferative
Cytostatic
Thiophene derivatives
title_short Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines
title_full Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines
title_fullStr Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines
title_full_unstemmed Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines
title_sort Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines
author Aguiar, Andreza Conception Véras de
author_facet Aguiar, Andreza Conception Véras de
Moura, Ricardo Olímpio de
Mendonça Junior, Jaime Francisco Bezerra
Rocha, Hugo Alexandre de Oliveira
Câmara, Rafael Barros Gomes da
Schiavon, Manuela dos Santos Carvalho
author_role author
author2 Moura, Ricardo Olímpio de
Mendonça Junior, Jaime Francisco Bezerra
Rocha, Hugo Alexandre de Oliveira
Câmara, Rafael Barros Gomes da
Schiavon, Manuela dos Santos Carvalho
author2_role author
author
author
author
author
dc.contributor.author.fl_str_mv Aguiar, Andreza Conception Véras de
Moura, Ricardo Olímpio de
Mendonça Junior, Jaime Francisco Bezerra
Rocha, Hugo Alexandre de Oliveira
Câmara, Rafael Barros Gomes da
Schiavon, Manuela dos Santos Carvalho
dc.subject.por.fl_str_mv Anticancer
Antiproliferative
Cytostatic
Thiophene derivatives
topic Anticancer
Antiproliferative
Cytostatic
Thiophene derivatives
description In spite of great progress in understanding cancer biology, current therapeutic procedures remain unsatisfactory. Chemotherapy is often followed by secondary effects with cellular toxicity negatively affecting the results. The discovery and development of new safe and efficient antitumor agents is necessary. Derivatives of 2-amino thiophene have been a topic of constant investigation due to their versatile synthetic applicability and broad spectrum of biological applications; among which are antifungal and antiproliferative activity shown in prior studies of our group. In the current study, compounds 6CN09, 6CN10, 6CN12, 6CN14, 7CN09 and 7CN11 were analyzed as to antiproliferative effect in human cells of cervical adenocarcinoma (HeLa), human pancreatic adenocarcinoma (PANC-1) and mice fibroblasts (3T3), which were exposed to the compounds in concentrations of 5, 10, 25 and 50mM during 24 and 48 h. They were submitted to MTT assay. In order to elucidate the action mechanism of antitumor thiophene derivatives flow cytometry was performed to evaluate cell death and cell cycle analysis. The results showed that thiophene derivatives demonstrated great antiproliferative potential in the HeLa and PANC-1 cell lines when compared with the control, and the percentage of cell proliferation inhibition approximated or was higher than the standard drug used; doxorubicin (Dox). In highlight were the derivatives 6CN14 and 7CN09 that showed greater efficiency in the antiproliferative evaluation. Further, all compounds had a protective effect on the non-tumor 3T3 cell line. The flow cytometry analysis showed few cells in apoptosis in both the HeLa and PANC-1 lines, although the compounds interfered with the progression of the cell cycle, and avoided cell growth and multiplication in the HeLa tumor line. These thiophene derivatives demonstrated cytostatic and antiproliferative effects and may be considered as promising molecular candidates for anticancer drugs
publishDate 2016
dc.date.issued.fl_str_mv 2016-12
dc.date.accessioned.fl_str_mv 2021-01-28T19:41:49Z
dc.date.available.fl_str_mv 2021-01-28T19:41:49Z
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.citation.fl_str_mv AGUIAR, Andreza Conception Véras de; MOURA, Ricardo Olímpio de; MENDONÇA, Jaime Francisco Bezerra; ROCHA, Hugo Alexandre de Oliveira; CÂMARA, Rafael Barros Gomes da; SCHIAVON, Manuela dos Santos Carvalho. Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines. Biomedicine & Pharmacotherapy, [s. l.], v. 84, p. 403-414, dez. 2016. Elsevier BV. Disponível em: https://www.sciencedirect.com/science/article/abs/pii/S0753332216312185?via%3Dihub. Acesso em: 04 ago. 2020. Http://dx.doi.org/10.1016/j.biopha.2016.09.026.
dc.identifier.uri.fl_str_mv https://repositorio.ufrn.br/handle/123456789/31316
dc.identifier.issn.none.fl_str_mv 0753-3322 (print)
dc.identifier.doi.none.fl_str_mv 10.1016/j.biopha.2016.09.026
identifier_str_mv AGUIAR, Andreza Conception Véras de; MOURA, Ricardo Olímpio de; MENDONÇA, Jaime Francisco Bezerra; ROCHA, Hugo Alexandre de Oliveira; CÂMARA, Rafael Barros Gomes da; SCHIAVON, Manuela dos Santos Carvalho. Evaluation of the antiproliferative activity of 2-amino thiophene derivatives against human cancer cells lines. Biomedicine & Pharmacotherapy, [s. l.], v. 84, p. 403-414, dez. 2016. Elsevier BV. Disponível em: https://www.sciencedirect.com/science/article/abs/pii/S0753332216312185?via%3Dihub. Acesso em: 04 ago. 2020. Http://dx.doi.org/10.1016/j.biopha.2016.09.026.
0753-3322 (print)
10.1016/j.biopha.2016.09.026
url https://repositorio.ufrn.br/handle/123456789/31316
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.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:Repositório Institucional da UFRN
instname:Universidade Federal do Rio Grande do Norte (UFRN)
instacron:UFRN
instname_str Universidade Federal do Rio Grande do Norte (UFRN)
instacron_str UFRN
institution UFRN
reponame_str Repositório Institucional da UFRN
collection Repositório Institucional da UFRN
bitstream.url.fl_str_mv https://repositorio.ufrn.br/bitstream/123456789/31316/2/license_rdf
https://repositorio.ufrn.br/bitstream/123456789/31316/3/license.txt
https://repositorio.ufrn.br/bitstream/123456789/31316/4/EvaluationAntiproliferativeActivity_C%c3%a2mara_2016.pdf.txt
https://repositorio.ufrn.br/bitstream/123456789/31316/5/EvaluationAntiproliferativeActivity_C%c3%a2mara_2016.pdf.jpg
bitstream.checksum.fl_str_mv 4d2950bda3d176f570a9f8b328dfbbef
e9597aa2854d128fd968be5edc8a28d9
dcf22f16d2e8855dc69f6e2886d7bfdf
033641a909af205a587448567709cbe9
bitstream.checksumAlgorithm.fl_str_mv MD5
MD5
MD5
MD5
repository.name.fl_str_mv Repositório Institucional da UFRN - Universidade Federal do Rio Grande do Norte (UFRN)
repository.mail.fl_str_mv
_version_ 1814832882242289664