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Structure-activity relationships of hypervalent organochalcogenanes as inhibitors of cysteine cathepsins V and S.
Piovan, Leandro; Alves, Márcio F M; Juliano, Luiz; Brömme, Dieter; Cunha, Rodrigo L O R; Andrade, Leandro H.
Afiliação
  • Piovan L; Instituto de Química, Universidade de São Paulo, Av. Prof. Lineu Prestes 748, SP 05508-900, São Paulo, Brazil.
Bioorg Med Chem ; 19(6): 2009-14, 2011 Mar 15.
Article em En | MEDLINE | ID: mdl-21345684
A new series of organotelluranes were synthesized and investigated, and the structure-activity relationships in cysteine proteases inhibition were determined. 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.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Proteases / Telúrio / Catepsinas Limite: Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2011 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Proteases / Telúrio / Catepsinas Limite: Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2011 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido