Bis-indole derivatives and pharmaceutical compositions containing them

摘要

The invention relates to novel bis-indole derivatives of the general formula (I) <IMAGE> (I) wherein R1 stands for a hydrogen atom or an acetyl group; R2 stands for a hydrogen atom; R3 means an ethyl group of alpha -position; or R2 and R3 together represent an oxygen bridge; R4 represents an ethyl or hydroxyl group of beta -position; and R5 stands for a hydrogen atom or a hydroxyl group; A represents a C1-10 straight-chain or C3-10 branched-chain alkyl group, hydroxy-alkyl, acetyl-alkyl, benzyl, C3-6 alkenyl or alkynyl or C5-7 cycloalkyl group or an aromatic group or a heteroaromatic group containing one nitrogen or one oxygen atom, and X stands for oxygen or sulphur atom, as well as their acid addition salts and pharmaceutical preparations containing these compounds. Further on, the invention relates to a process for preparing these compounds and preparations. The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.