Camptothecin with a modified lactone ring

Abstract

Compound: of formula (II) where: R1 is hydrogen or a -C(R5)=N-O-R4 group, in which R4 is hydrogen or a straight or branched C1-C5 alkyl or C1-C5 alkenyl group, or a C3-C10 cycloalkyl group, or a straight or branched (C3-C10) cycloalkyl - (C1-C5) alkyl group, or a C6-C14 aryl group, or a straight or branched (C6-C14) aryl - (C1-C5) alkyl group, or a heterocyclic group or a straight or branched. heterocyclo - (C1-C5) alkyl group, said heterocyclic group containing at least one beteroatoin selected from an atom of nitrogen, optionally substituted with an (C1-C5) alkyl group, and / or an atom of oxygen and / or of sulphur; said alkyl, alkenyl, cycloalkyl, cycloalkyl¬alkyl, aryl, aryl-alkyl, heterocyclic or heterocyclo-alkyl groups can optionally be substituted with one or more groups selected from the group consisting of: halogen, hydroxy, C1-C5 alkyl, C1-C5 alkoxy, phenyl, cyano, nitro, and -NR6R7, where R6 and R7, which may be the same or different, are hydrogen, straight or branched (C1-C5) alkyl, the -COOH group or one of its pharmaceutically acceptable esters; or the – CONR8R9 group, where R8 and R9, which may be the same or different, are hydrogen, straight or branched (C1-C5) alkyl; or R4 is a (C5-C10) aroyl or (C6-C10) arylsulphonyl residue, optionally substituted with one or more groups selected from: halogen, hydroxy, straight or branched C1-C5 alkyl, straight or branched C1-C5 alkoxy, phenyl, cyano, nitro, -NR10R11, where R10 and R11, which may be the same or different, are hydrogen, straight or branched C1-C5 alkyl; or: R4 is a polyaminoalkyl residue; or R4 is a glycosyl residue; R5 is hydrogen, straight or branched C1-C5 alkyl, straight or branched C1-C5 alkenyl, C3-C1 cyloalkyl, straight or branched (C3-C10) cycloalkyl - (C1-C5) alkyl, C6-C14 aryl, straight or branched (C1-C5) aryl - (C1-C5) alkyl; R2 and. R3 which may be the same or different, are hydrogens, hydroxy, straight or branched C1-C5 alkoxy; n=1 or 2, Z is selected from hydrogen straight or branched C – C alkyl; with the proviso that in formula (II) R4, R2 and R3 cannot be simultaneously hydrogen.