Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S

Detalhes bibliográficos
Autor(a) principal: Piovan, Leandro
Data de Publicação: 2011
Outros Autores: Alves, Marcio Fernando [UNIFESP], Juliano, Luiz [UNIFESP], Broemme, Dieter, Cunha, Rodrigo Luiz Oliveira Rodrigues [UNIFESP], Andrade, Leandro H.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UNIFESP
Texto Completo: http://repositorio.unifesp.br/handle/11600/33556
http://dx.doi.org/10.1016/j.bmc.2011.01.054
Resumo: A new series of organotelluranes were synthesized and investigated, and the structure-activity relationships in cysteine proteases inhibition were determinated. It was possible to identify the relevance of structural components linked to the reactivity of these compounds as inhibitors. for example, dibromo-organotelluranes showed to be more reactive than dichloro-organotelluranes towards cysteine cathepsins V and S. Besides, no remarkable enantio-selectivity was verified. in general the achiral organotelluranes were more reactive than the chiral congeners against cysteine cathepsins V and S. A reactivity order for organochalcogenanes and cysteine cathepsins was proposed after the comparison of the inhibitory potencies of organotelluranes with the related organoselenanes. (C) 2011 Elsevier B.V. All rights reserved.
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spelling Piovan, LeandroAlves, Marcio Fernando [UNIFESP]Juliano, Luiz [UNIFESP]Broemme, DieterCunha, Rodrigo Luiz Oliveira Rodrigues [UNIFESP]Andrade, Leandro H.Universidade Federal de São Paulo (UNIFESP)Universidade de São Paulo (USP)Univ British ColumbiaUniversidade Federal do ABC (UFABC)2016-01-24T14:06:18Z2016-01-24T14:06:18Z2011-03-15Bioorganic & Medicinal Chemistry. Oxford: Pergamon-Elsevier B.V., v. 19, n. 6, p. 2009-2014, 2011.0968-0896http://repositorio.unifesp.br/handle/11600/33556http://dx.doi.org/10.1016/j.bmc.2011.01.054WOS000288196900018.pdf10.1016/j.bmc.2011.01.054WOS:000288196900018A new series of organotelluranes were synthesized and investigated, and the structure-activity relationships in cysteine proteases inhibition were determinated. It was possible to identify the relevance of structural components linked to the reactivity of these compounds as inhibitors. for example, dibromo-organotelluranes showed to be more reactive than dichloro-organotelluranes towards cysteine cathepsins V and S. Besides, no remarkable enantio-selectivity was verified. in general the achiral organotelluranes were more reactive than the chiral congeners against cysteine cathepsins V and S. A reactivity order for organochalcogenanes and cysteine cathepsins was proposed after the comparison of the inhibitory potencies of organotelluranes with the related organoselenanes. (C) 2011 Elsevier B.V. All rights reserved.Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Universidade Federal de São Paulo, Dept Biofis, Escola Paulista Med, BR-04044200 São Paulo, BrazilUniv São Paulo, Inst Quim, BR-05508900 São Paulo, BrazilUniv British Columbia, Dept Dent, Fac Dent, Vancouver, BC V6T 1Z3, CanadaUniv British Columbia, UBC Ctr Blood Res, Fac Dent, Vancouver, BC V6T 1Z3, CanadaUniv Fed ABC, CCNH, BR-09210580 Santo Andre, SP, BrazilUniversidade Federal de São Paulo, Dept Biofis, Escola Paulista Med, BR-04044200 São Paulo, BrazilWeb of Science2009-2014engElsevier B.V.Bioorganic & Medicinal Chemistryhttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policyinfo:eu-repo/semantics/openAccessTelluriumSeleniumCathepsinIinhibitionStructure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and Sinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlereponame:Repositório Institucional da UNIFESPinstname:Universidade Federal de São Paulo (UNIFESP)instacron:UNIFESPORIGINALWOS000288196900018.pdfapplication/pdf907022${dspace.ui.url}/bitstream/11600/33556/1/WOS000288196900018.pdf71f785cdc5d990d2b4d12468504a44d3MD51open accessTEXTWOS000288196900018.pdf.txtWOS000288196900018.pdf.txtExtracted texttext/plain28691${dspace.ui.url}/bitstream/11600/33556/2/WOS000288196900018.pdf.txte6acc9a46300e2100db6179908aef936MD52open access11600/335562022-09-27 10:00:03.139open accessoai:repositorio.unifesp.br:11600/33556Repositório InstitucionalPUBhttp://www.repositorio.unifesp.br/oai/requestopendoar:34652023-05-25T12:24:18.619780Repositório Institucional da UNIFESP - Universidade Federal de São Paulo (UNIFESP)false
dc.title.en.fl_str_mv Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S
title Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S
spellingShingle Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S
Piovan, Leandro
Tellurium
Selenium
Cathepsin
Iinhibition
title_short Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S
title_full Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S
title_fullStr Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S
title_full_unstemmed Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S
title_sort Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S
author Piovan, Leandro
author_facet Piovan, Leandro
Alves, Marcio Fernando [UNIFESP]
Juliano, Luiz [UNIFESP]
Broemme, Dieter
Cunha, Rodrigo Luiz Oliveira Rodrigues [UNIFESP]
Andrade, Leandro H.
author_role author
author2 Alves, Marcio Fernando [UNIFESP]
Juliano, Luiz [UNIFESP]
Broemme, Dieter
Cunha, Rodrigo Luiz Oliveira Rodrigues [UNIFESP]
Andrade, Leandro H.
author2_role author
author
author
author
author
dc.contributor.institution.none.fl_str_mv Universidade Federal de São Paulo (UNIFESP)
Universidade de São Paulo (USP)
Univ British Columbia
Universidade Federal do ABC (UFABC)
dc.contributor.author.fl_str_mv Piovan, Leandro
Alves, Marcio Fernando [UNIFESP]
Juliano, Luiz [UNIFESP]
Broemme, Dieter
Cunha, Rodrigo Luiz Oliveira Rodrigues [UNIFESP]
Andrade, Leandro H.
dc.subject.eng.fl_str_mv Tellurium
Selenium
Cathepsin
Iinhibition
topic Tellurium
Selenium
Cathepsin
Iinhibition
description A new series of organotelluranes were synthesized and investigated, and the structure-activity relationships in cysteine proteases inhibition were determinated. It was possible to identify the relevance of structural components linked to the reactivity of these compounds as inhibitors. for example, dibromo-organotelluranes showed to be more reactive than dichloro-organotelluranes towards cysteine cathepsins V and S. Besides, no remarkable enantio-selectivity was verified. in general the achiral organotelluranes were more reactive than the chiral congeners against cysteine cathepsins V and S. A reactivity order for organochalcogenanes and cysteine cathepsins was proposed after the comparison of the inhibitory potencies of organotelluranes with the related organoselenanes. (C) 2011 Elsevier B.V. All rights reserved.
publishDate 2011
dc.date.issued.fl_str_mv 2011-03-15
dc.date.accessioned.fl_str_mv 2016-01-24T14:06:18Z
dc.date.available.fl_str_mv 2016-01-24T14:06:18Z
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 Bioorganic & Medicinal Chemistry. Oxford: Pergamon-Elsevier B.V., v. 19, n. 6, p. 2009-2014, 2011.
dc.identifier.uri.fl_str_mv http://repositorio.unifesp.br/handle/11600/33556
http://dx.doi.org/10.1016/j.bmc.2011.01.054
dc.identifier.issn.none.fl_str_mv 0968-0896
dc.identifier.file.none.fl_str_mv WOS000288196900018.pdf
dc.identifier.doi.none.fl_str_mv 10.1016/j.bmc.2011.01.054
dc.identifier.wos.none.fl_str_mv WOS:000288196900018
identifier_str_mv Bioorganic & Medicinal Chemistry. Oxford: Pergamon-Elsevier B.V., v. 19, n. 6, p. 2009-2014, 2011.
0968-0896
WOS000288196900018.pdf
10.1016/j.bmc.2011.01.054
WOS:000288196900018
url http://repositorio.unifesp.br/handle/11600/33556
http://dx.doi.org/10.1016/j.bmc.2011.01.054
dc.language.iso.fl_str_mv eng
language eng
dc.relation.ispartof.none.fl_str_mv Bioorganic & Medicinal Chemistry
dc.rights.driver.fl_str_mv http://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
info:eu-repo/semantics/openAccess
rights_invalid_str_mv http://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 2009-2014
dc.publisher.none.fl_str_mv Elsevier B.V.
publisher.none.fl_str_mv Elsevier B.V.
dc.source.none.fl_str_mv reponame:Repositório Institucional da UNIFESP
instname:Universidade Federal de São Paulo (UNIFESP)
instacron:UNIFESP
instname_str Universidade Federal de São Paulo (UNIFESP)
instacron_str UNIFESP
institution UNIFESP
reponame_str Repositório Institucional da UNIFESP
collection Repositório Institucional da UNIFESP
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