abstract |
FIELD: synthesis of biologically active compounds. n SUBSTANCE: invention relates to varioline derivatives of general formula (5a), wherein R1 is selected from halogen and C 1 -C 12 -alkyl; R 2 is selected from hydrogen and halogen; R 3 , R 4 , R 5 , R 6 , and R 7 represent hydrogen; X 1 amino group optionally substituted by C 1 -C 12 -alkoxy, benzylamino, C 1 -C 12 -alkylsulfinyl, or C 1 -C 12 -thioalkyl; X 2 amino group, C 1 -C 12 -thioalkyl, C 1 -C 12 -alkylsulfinyl, or optionally C 1 -C 12 -alkoxy-substituted benzylamino; or R 1 and R 2 pair can be combined into condensed benzene ring system optionally substituted by C 1 -C 12 -alkoxy group. Indicated compounds exhibit antitumor activity. Invention further relates to pharmaceutical composition based on these compounds and use of these compounds to prepare drug useful in treatment of cancer. Invention also comprises a method for preparing intermediate varioline compounds. . n EFFECT: expanded synthetic possibilities in heterocyclic compounds area and increased choice of antitumor agents. n 16 cl, 107 ex |