发明名称 C7-ESTER-SUBSTITUTED TAXANES AS ANTI-TUMOR AGENTS
摘要 FIELD: organic chemistry of natural compounds, medicine, oncology. ^ SUBSTANCE: invention relates to new compounds - C7-ester-substituted taxanes of the general structural formula: ^ wherein R2 represents benzoyloxy-group; R7 represents R7aCOO-; R10 represents hydroxy-group; X3 represents (C1-C8)-alkyl, (C2-C8)-alkenyl, (C2-C8)-alkynyl or 5- or 6-membered heteroaryl group comprising heteroatom taken among oxygen (O), nitrogen (N) and sulfur (S) atoms; X5 represents -COX10 wherein X10 represents (C1-C8)-alkyl, (C2-C8)-alkenyl, phenyl or 5- or 6-membered heteroaryl group comprising heteroatom taken among O, N and S; or it (X5) represents -COOX10 wherein X10 represents (C1-C8)-alkyl or (C2-C8)-alkenyl; R7a represents (C1-C20)-alkyl or (C2-C20)-alkenyl; Ac represents acetyl group. These compounds possess an anti-tumor activity. Also, invention relates to a method for inhibition of tumor growth in mammals and to a pharmaceutical composition based on synthesized compounds. Invention provides preparing new derivatives of taxanes possessing the enhanced anti-tumor activity and reduced toxicity as compared with taxol and taxoter. ^ EFFECT: improved and valuable medicinal properties of compounds. ^ 39 cl, 4 tbl, 10 ex
申请公布号 RU2265017(C2) 申请公布日期 2005.11.27
申请号 RU20010129507 申请日期 2001.02.02
申请人 发明人 KHOLTON ROBERT A.
分类号 A61K31/337;A61K31/341;A61K31/381;A61K31/4427;A61P35/00;C07D305/14;C07D405/12;C07D407/12;C07D409/12;C07D417/12 主分类号 A61K31/337
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