N-(VINBLASTINOYL-23) DERIVATIVES OF AMINO ACIDS, THEIR PREPARATION AND THERAPEUTICAL APPLICATION

摘要

Vinblastine derivatives of the general formula: wherein R is an ester of an amino-acid which is possibly protected, attached to the vinblastin-23-oyl moiety by an amide bond, the ester group, which may be straight or branched, containing 2-9 carbon atoms and R1 is a hydrogen atom or a hydroxy group, R2 is a hydrogen atom, a formyl group or a C2-C9 acyl group, R5 is a hydrogen atom or a methyl group or a formyl group, with the provision that compounds where R5 is methyl and R1 is a beta -hydroxy group are excluded; or their addition salts with mineral or organic acids. The compounds are useful as drugs.