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ID: ALA1132101

Journal: Bioorg Med Chem Lett

Title: Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors.

Authors: Dumas J, Brittelli D, Chen J, Dixon B, Hatoum-Mokdad H, König G, Sibley R, Witowsky J, Wong S.

Abstract: Cathepsin D, a lysosomal aspartyl protease, has been implicated in the pathology of Alzheimer's disease as well as breast and ovarian cancer. A weakly active cathepsin D inhibitor was identified by high throughput screening. Subsequent optimization led to the discovery of a new class of small molecule inhibitors of this enzyme, culminating with the sulfonamide 13 (IC50 = 250 nM).

CiteXplore: 10498202

DOI: 10.1016/s0960-894x(99)00433-3