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

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

Author Piovan, Leandro Google Scholar
Alves, Marcio Fernando Autor UNIFESP Google Scholar
Juliano, Luiz Autor UNIFESP Google Scholar
Broemme, Dieter Google Scholar
Cunha, Rodrigo Luiz Oliveira Rodrigues Autor UNIFESP Google Scholar
Andrade, Leandro H. Google Scholar
Institution Universidade Federal de São Paulo (UNIFESP)
Universidade de São Paulo (USP)
Univ British Columbia
Universidade Federal do ABC (UFABC)
Abstract 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.
Keywords Tellurium
Selenium
Cathepsin
Iinhibition
Language English
Sponsor 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)
Date 2011-03-15
Published in Bioorganic & Medicinal Chemistry. Oxford: Pergamon-Elsevier B.V., v. 19, n. 6, p. 2009-2014, 2011.
ISSN 0968-0896 (Sherpa/Romeo, impact factor)
Publisher Elsevier B.V.
Extent 2009-2014
Origin http://dx.doi.org/10.1016/j.bmc.2011.01.054
Access rights Open access Open Access
Type Article
Web of Science ID WOS:000288196900018
URI http://repositorio.unifesp.br/handle/11600/33556

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