Cytostatic beta-carbolines

Abstract

The invention relates to a group of new .beta.-carbolines, their bio-isosteric benzofuran and benzothiophene analogues, and to the preparation of these compounds. The new compounds can be represented by the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are hydrogen, or R+R.sub.1 or R.sub.1 +R.sub.2 form a saturated heterocyclic ring having 5 or 6 ring atoms, which comprise 1 or 2 oxygen atoms; R.sub.3 is hydrogen, or hydroxy optionally derivatised with a sugar radical the 4,6-hydroxy groups of which are acetalised with an -ylidene group; R.sub.4 is a group of the formula --C(R.sub.11).sub.2 --X--R.sub.12, wherein the groups R.sub.11 are hydrogen, or both groups R.sub.11 together represent a double-bonded keto oxygen atom, X is oxygen or a group NR.sub.14, wherein R.sub.14 is hydrogen or alkyl having 1-4 C-atoms, and R.sub.12 is hydrogen, alkyl having 1-4 C-atoms, alkanoyl having 1-4 C-atoms, the carbamoyl group or mono- or dialkylcarbamoyl group having 1-4 C-atoms per alkyl group; R.sub.5 is hydrogen, alkanoyl or alkyl having 1-4 C-atoms, or R.sub.4 +R.sub.5 together form a group of the formula --C(R.sub.11).sub.2 --X--Z, wherein R.sub.11 and X have the above-mentioned meanings and Z is bound to the ring nitrogen atom and is a group ##STR2## R.sub.7 and R.sub.9 independently of each other are hydrogen or alkoxy having 1-4 C-atoms, trifluoromethyl or halogen; R.sub.8 is hydrogen, alkoxy or alkanoyloxy having 1-4 C-atoms, hydroxy, halogen, benzyloxy, or R.sub.8 and R.sub.9 together constitute a dioxyalkylidene bridge; A is oxygen, sulphur or a group ##STR3## and R.sub.6 and R.sub.13 independently of each other are hydrogen or methyl, or, when A is nitrogen, R.sub.6 and R.sub.13 together may form a ring having 5-7 C-atoms. The compounds have good cytostatic properies.

Dependencies are inferred from the claim text.