proteinkonjugater of bis indole alkaloids, bis indole alkaloids, their manufacture and use

摘要

A protein conjugate of bis-indole alkaloids having the formula (I) Ar-N=N-bisindole alkaloid, wherein Ar is a benzoe- or arylalkylcarboxylic acid group which contains a protein group. The invention also concerns a process for the preparation of a protein conjugate of bis-indole alkaloids having the formula (I), in which process is reacted with a diazonium acid derivative having the formula Ar-N=N(+), wherein Ar represents the same as above with the exception, however, that Ar may not contain a protein group in which case a protein group is attached to an aromatic acid group. The invention further concerns a bis-indole alkaloid derivative, having the formula Ar1-N=N-bis-indole alkaloid, wherein Ar1 represents a benzoe-or arylalkylcarboxylic acid group. Said derivative is useful compound in preparation of the conjugates of formula (I). Finally conjugates of formula (I) in immunometric methods and in the treatment of diseases, especially cancer.