| 摘要 |
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 <CHEM> wherein - R, R1 and R2 are hydrogen, or R + R1 or R1 + R2 form a saturated heterocyclic ring having 5 or 6 ring atoms, which comprise 1 or 2 oxygen atoms; -R3 is hydrogen, or hydroxy optionally derivatised with a sugar radical the 4,6-hydroxy groups of which are acetalised with an -ylidene group; -R4 is a group of the formula -C(R11)2-X-R12, wherein the groups R11 are hydrogen, or both groups R11 together represent a double-bonded keto oxygen atom, X is oxygen or a group NR14, wherein R14 is hydrogen or alkyl having 1-4 Catoms, and R12 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; -R5 is hydrogen, alkanoyl or alkyl having 1-4 C-atoms, or R4 + R5 together form a group of the formula -C(R11)2-X-Z, wherein R11 and X have the above-mentioned meanings and Z is bound to the ring nitrogen atom and is a group @C=O,@C=S, @S->O or <CHEM> - R7 and R9 independently of each other are hydrogen or alkoxy having 1-4 C-atoms, trifluoromethyl or halogen; - R8 is hydrogen, alkoxy or alkanoyloxy having 1-4 C-atoms, hydroxy, halogen, benzyloxy, or R8 and R9 together constitute a dioxyalkylidene bridge; - A is oxygen, sulphur or a group @NR6, and - R6 and R13 independently of each other are hydrogen or methyl, or, when A is nitrogen, R6 and R13 together may form a ring having 5-7 C-atoms. The compounds have good cytostatic properies. |
