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Beilstein J. Org. Chem. 2013, 9, 15–25, doi:10.3762/bjoc.9.3
Graphical Abstract
Figure 1: Chemical structures of vinylsulfone-based cruzain inhibitors 1–4, known TcCYP51 inhibitor 5, dihydr...
Figure 2: Computational docking models. (A) Predicted binding modes of 4 and (R)-5 bound to TcCYP51. For 4, t...
Figure 3: Synthesis of the additional control compound 6–8, the reduced forms of analogues 1, 3, and 4 respec...
Figure 4: GC/MS analysis of lipid extracts from T. cruzi parasites treated with test compounds. DMSO and K777...
Figure 5: Chemical structures of compound 9, a “clickable” activity-based probe based on 1 and complementary ...
Figure 6: Competitive labeling of host cell (C2C12) proteins. Intact cells were labeled with probe 9 followin...
Figure 7: MS/MS spectrum of the tryptic peptide S264-R281 from mouse cathepsin B, identified in pull-down exp...