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Bioorg. Med. Chem. Lett. · Jun 2008
Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype.
- Michael C Myers, Parag P Shah, Mary Pat Beavers, Andrew D Napper, Scott L Diamond, Amos B Smith, and Donna M Huryn.
- Penn Center for Molecular Discovery, University of Pennsylvania, 1024 Vagelos Research Laboratories, Philadelphia, PA 19104-6383, USA.
- Bioorg. Med. Chem. Lett. 2008 Jun 15; 18 (12): 3646-51.
AbstractRecently, 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.
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