CPC C07K 7/64 (2013.01) [A61K 47/6831 (2017.08); A61K 38/00 (2013.01)] | 20 Claims |
1. An amanitin derivative comprising a hydroxylated tryptophan moiety, which is selected from (i) S-desoxy-4′-hydroxy-amanin, 4′-hydroxy-amanin, S-desoxy-5′-hydroxy-amanin, 5′-hydroxy-amanin, S-desoxy-7′-hydroxy-amanin, 7′-hydroxy-amanin, (ii) S-desoxy-4′-hydroxy-amaninamide, 4′-hydroxy-amaninamide, S-desoxy-5′-hydroxy-amaninamide, 5′-hydroxy-amaninamide, S-desoxy-7′-hydroxy-amaninamide, and 7′-hydroxy-amaninamide, and (iii) a derivative of the amanitin according to (i), wherein the free carboxylic acid moiety of amino acid 1 is converted to a carboxylic ester —C(═O)OR1 or to a moiety —C(═O)NH—OR1, wherein R1 is selected from alkyl, aryl, heteroaryl, substituted alkyl, substituted aryl, and substituted heteroaryl, and wherein amino acid 1 is positioned between the cysteinyl residue and the hydroxy-prolyl residue of the amanitin derivative.
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