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ID: ALA1145569

Journal: Bioorg Med Chem Lett

Title: Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype.

Authors: Myers MC, Shah PP, Beavers MP, Napper AD, Diamond SL, Smith AB, Huryn DM.

Abstract: Recently, we identified a thiocarbazate that exhibits potent inhibitory activity against human cathepsin L. Since this structure represents a novel chemotype with potential for activity against the entire cysteine protease family, we designed, synthesized, and assayed a series of analogs to probe the mechanism of action, as well as the structural requirements for cathepsin L activity. Molecular docking studies using coordinates of a papain-inhibitor complex as a model for cathepsin L provided useful insights.

CiteXplore: 18499453

DOI: 10.1016/j.bmcl.2008.04.065