OPTICALLY PURE ANALOGS OF CAMPTOTHECIN Russian patent published in 2004 - IPC

FIELD: organic chemistry, biochemistry, medicine.

SUBSTANCE: invention relates, in particular, to new compounds of the general formula (I_A):

wherein radical R₁ means lower alkyl radical; R₂, R₃, R₄ and R₅ mean independently hydrogen atom, halide radical or -OSO₂R₁₀; R₆ means hydrogen atom, linear or branched alkyl radical with 1-12 carbon atoms possibly substituted with one or some similar or different halide radicals, lower hydroxyalkyl (lower alkoxy)-(lower alkyl), cycloalkyl, cycloalkyl(lower alkyl), halogen atom, group -(CH₂)_mSiR₇R₈R₉, substituted or unsubstituted aryl, or substituted or unsubstituted aryl(lower alkyl) being one or some similar or different substituents and aryl groups are taken among the following radicals: lower alkyl, halogen atom, amino-group, (lower alkyl)-amino-group, di-(lower alkyl)-amino-group, CF₃ or OCF₃; R₇, R₈ and R₉ mean independently lower alkyl radical; R₁₀ means lower alkyl radical possibly substituted with one or some similar or different halide radicals; m means a whole number from 0 to 6. These compounds are inhibitors of topoisomerases and represent the specific interest as medicinal agents eliciting anti-tumor activity.

EFFECT: valuable medicinal properties of compounds.

1 tbl, 90 ex