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ID: ALA1681765

Journal: Bioorg Med Chem

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

Authors: Piovan L, Alves MF, Juliano L, Brömme D, Cunha RL, Andrade LH.

Abstract: 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.

CiteXplore: 21345684

DOI: 10.1016/j.bmc.2011.01.054