VARIOLINE DERIVATIVES AND THEIR EMPLOYMENT AS ANTITUMOR AGENTS Russian patent published in 2007 - IPC C07D471/04 A61K31/519 A61P35/00 C07D401/14 C07D401/06 

Abstract RU 2302419 C2

FIELD: synthesis of biologically active compounds.

SUBSTANCE: invention relates to varioline derivatives of general formula (5a), wherein R1 is selected from halogen and C1-C12-alkyl; R2 is selected from hydrogen and halogen; R3, R4, R5, R6, and R7 represent hydrogen; X1 amino group optionally substituted by C1-C12-alkoxy, benzylamino, C1-C12-alkylsulfinyl, or C1-C12-thioalkyl; X2 amino group, C1-C12-thioalkyl, C1-C12-alkylsulfinyl, or optionally C1-C12-alkoxy-substituted benzylamino; or R1 and R2 pair can be combined into condensed benzene ring system optionally substituted by C1-C12-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. .

EFFECT: expanded synthetic possibilities in heterocyclic compounds area and increased choice of antitumor agents.

16 cl, 107 ex

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Authors

Remuin'Jan Modesto

Gonsales Khuan Khose

Del' Poso Karlos

Fransesch Andres

Kuehvas Karmen

Mant Sajmon

Mansanares Ignasio

Anderson Rigan Dzhejms

Morris Dzhonatan Charl'Z

Dates

2007-07-10Published

2002-07-11Filed