Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S
Autor(a) principal: | |
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Data de Publicação: | 2011 |
Outros Autores: | , , , , |
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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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:34652022-09-27T13:00:03Repositório 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. |
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