| abstract |
The invention relates to a compound of the following general formula (tubulysin) n n nhaving 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: n 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, alkyl or a metal ion V=H, OR 7 , Hal or (for W=O)O R 7 =H, C 1-4 alkyl or COR 8 R5=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 free electron pair) CH 3 or (for Y=free electron pair) COR 11 . |