A good imitation: Aryl‐1‐indanyl ketones are found to be highly efficient, reversible, cell‐penetrating inhibitors of the human peptidyl prolyl cis/trans isomerase Pin1. Owing to their structure 1, ...they are assumed to mimic the transition state 2 of the enzymatically catalyzed rotation about the imidic peptide bond preceding a proline residue.
The novel 3H-spiro1-benzofuran-2-cyclopentan-3-one skeleton has been made accessible by different routes. One- and two-step protocols lead to tricyclic and tetracyclic benzofuranones 2 and 3, ...respectively. A four-step synthesis to spirocompound 4 is described. The novel spirocyclic benzofuranones display modest to no inhibition of the human peptidyl prolyl cis/trans isomerase Pin1.
The treatment of the 5-(phenylsulfinyl)indoles with trifluoroacetic anhydride in the presence of carbon nucleophiles achieved the title reactions with complete regioselectivity.
The treatment of the ...5-(phenylsulfinyl)indoles with trifluoroacetic anhydride in the presence of carbon nucleophiles achieved the title reactions with complete regioselectivity.
A simple, mild and high-yielding procedure for the reduction of various halogenated compounds using a combination of the water-soluble radical initiater (VA-061), hypophosphorous acid and ...triethylamine in aqueous alcohol is reported.
A simple, mild, and high-yielding procedure for the reduction of various halogenated compounds using a combination of the water-soluble radical initiator, 2,2′-azobis2-(2-imidazolin-2-yl)propane (VA-061), a water-soluble chain carrier, hypophosphorous acid, and the base, triethylamine, in aqueous alcohol is described. The reagents used in this method are all water soluble, and therefore, an almost pure desired product can be readily obtained using only an extraction procedure.
Geschickt imitiert: Aryl‐1‐indanylketone erweisen sich als hocheffiziente, reversible und zellgängige Inhibitoren der humanen Peptidyl‐Prolyl‐cis/trans‐Isomerase Pin1. Aufgrund ihrer Struktur 1 wird ...angenommen, dass sie den Übergangszustand 2 der enzymatisch katalysierten Rotation um die imidische Peptidbindung vor dem Prolin nachahmen.
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