| abstract |
The invention relates to novel substituted noscapine derivatives of general formula (1) or to the racemates or to optical isomers or to the pharmaceutically acceptable salts and/or hydrates thereof exhibiting antitumor activity, to a pharmaceutical composition in the form of tablets, capsules or injections placed into pharmaceutically acceptable packages, to methods for the production thereof and to a method for inhibiting proliferation with the use thereof. According to general formula (1) R1 is an aminogroup substituent selected from alkyl; R2 is a cyclic system substituent selected from possibly substituted alkyl, wherein the substituents are selected from a possibly substituted aminogroup or azaheterocycle which possibly contains O, S or N in the form of an additional heteroatom and linked to an alkyl group by a nitrogen atom, from possibly substituted aryl, possibly substituted and possibly condensed heteroaryl containing at least one heteroatom selected from nitrogen, sulphur and oxygen and from possibly substituted sulphamoil. The invention also relates to 3-(9-iodo-4-metoxy-6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo-[4,5-g]isoquinoline-5-il)-6,7-dimetoxy-3H- isobenzofuran-1, 3-(9-chloromethyl-4-metoxy-6-methyl-5,6,7,8-tetrahydro [1,3]dioxolo-[4,5-g] isoquinoline-5-il)-6,7-dimetoxy-3H-isobenzofuran-1, 5-(4,5-dimetoxy-3-oxo- 1,3-dihydroisonenzofuran-1-il) -4-metoxy-6-methyl-5,6,7,8-tetrahydro [1,3]dioxolo-[4,5-g] isoquinoline-carbaldehyde (or-9-carbonitril, or -9-sulphonylchloride, or -9-carboxylic acid and to 3-(9-metoxymethyl-métoxy-6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo-[4,5-g]isoquinoline-5-il)-6,7-dimetoxy-3H- isobenzofuran-1 and to the methods for the production thereof. Combinatory and focused libraries are also disclosed. |