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Beilstein J. Org. Chem. 2017, 13, 2869–2882, doi:10.3762/bjoc.13.279
Graphical Abstract
Figure 1: (a) Structures of isoleucine (1), leucine (2), and their fluorinated analogues 5,5,5-trifluoroisole...
Figure 2: Percentage of substrate remaining after incubation for 120 min (left) and 24 h (right) with α-chymo...
Figure 3: Cleavage positions observed in the digestion of library peptides with α-chymotrypsin.
Figure 4: Percentage of substrate remaining after incubation for 120 min (left) and 24 h (right) with pepsin ...
Figure 5: Cleavage positions for digestion of the different peptides with pepsin.
Figure 6: Percentage of substrate remaining after incubation for 120 min (left) and 24 h (right) with elastas...
Figure 7: Cleavage positions for digestion of the different peptides with elastase.
Figure 8: Percentage of substrate remaining after incubation for 120 min (left) and 24 h (right) with protein...
Figure 9: Cleavage positions found with proteinase K.
Figure 10: Dimension of stabilization or destabilization upon TfIle or HfLeu incorporation compared to the non...
Beilstein J. Org. Chem. 2014, 10, 1564–1569, doi:10.3762/bjoc.10.161
Figure 1: Structures of cyclopamine (1) and carbacyclopamine analog 2.
Scheme 1: Retrosynthetic analysis of carbacyclopamine analog 2.
Scheme 2: Synthesis of carbacyclopamine analog 2.
Beilstein J. Org. Chem. 2013, 9, 2328–2335, doi:10.3762/bjoc.9.267
Figure 1: Structures of cyclopamine and exo-cyclopamine.
Scheme 1: Synthesis of 25-epi-exo-cyclopamine 5, bis-exo-cyclopamine 6, and derivatives 8 and 9. Reaction con...
Scheme 2: Synthesis of 20-demethyl-bis-exo-cyclopamine 19 and F-nor-20,25-bis-demethyl-exo-cyclopamine 23. Re...
Figure 2: IC50 values of Shh inhibition by compounds 5, 6 and 23 in a Gli1-reporter gene assay. Data were obt...