| abstract |
The invention relates to a compound of the following general formula (tubulysin): with the following meanings for R, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , S, T, U, V, W, X, Y and Z: R = H, C 1-4 alkyl, aryl, OR 1 , NR 1 R 2 or NH- (CH 2 ) 2-4 - R 1 = H, C 1-6 alkyl or aryl R 2 = H, C 1-6 alkyl or aryl S = H, Hal, NO 2 or NHR 3 U = H, Hal, NO 2 or NHR 3 R 3 = H, HCO or C 1-4 alkyl CO T = H or OR 4 R 4 = H, C 1-4 alkyl, aryl, COR 5 , P (O) (OR 6 ) 2 or SO 3 R 6 R 5 = C 1-6 alkyl, alkenyl, aryl or heteroaryl R 6 = H, C 1-4 alkyl or metal ion V = H or R 7 or (for W = O) O R 7 = H, C 1-4 alkyl or COR 8 R 8 = C 1-4 alkyl, alkenyl or aryl W = H or C 1-4 alkyl or (for V = O) O X = H, C 1-4 alkyl, alkenyl or CH 2 OR 9 R 9 = H, C 1-4 alkyl, alkenyl, aryl or COR 10 R 10 = C 1-6 alkyl, alkenyl, aryl or heteroaryl Y = (for Z = CH 3 or COR 11 ) free electron pair or (for Z = CH 3 ) O R 11 = C 1-4 alkyl, CF 3 or aryl and / or Z = (for Y = O or lone pair) CH 3 or (for Y = lone pair) COR 11 . |