DERIVATIVES OF O-ALKYLGUANINE AND PHARMACEUTICAL COMPOSITION Russian patent published in 2000 - IPC

FIELD: organic chemistry, heterocyclic compounds, pharmacy. SUBSTANCE: invention describes the novel derivatives of O⁶-guanine of the general formula (I) where Y means hydrogen atom, ribosyl or deoxypibosyl that can be substituted with hydroxy- or C₁-C₄-aklkoxy-groups; R¹ means hydrogen atom, C_1-20-alkyl or hydroxy-C_1-20-alkyl; R means: (i) cyclic group containing five-membered ring with at least one heteroatom taken among O, N or S and optionally condensed with benzene, pyridine or naphthalene ring or six-membered heterocyclic ring containing at least one N-atom, optionally with S-atom, optionally condensed with one or two benzene rings where indicated cyclic group can be optionally substituted in heterocyclic ring(s) and/or carbocyclic ring(s) with groups taken among C₁-C₅-alkyl, halogen atom, cyano-, nitro-, azido-group, C₁-C₅-alkoxy-group, aryl, SO_nR″″ where R″″ means C₁-C₅-alkyl and n = 0, 1, 2, COOR⁵ where R⁵ means H or C₁-C₅-alkyl or N-oxides. Indicated compounds show ability to decrease activity of O⁶-alkylguanine DNA-alkyltransferase in tumor cells. Their activity is 8-fold above that of the known analogs. Invention describes also the composition based on compounds of the formula (I). EFFECT: new compounds indicated above, valuable biochemical and antitumor properties. 14 cl, 14 dwg, 7 tbl