Deletion of the oxetane ring in docetaxel analogues:: Synthesis and biological evaluation

被引:13
|
作者
Deka, V [1 ]
Dubois, J [1 ]
Thoret, S [1 ]
Guéritte, F [1 ]
Guénard, D [1 ]
机构
[1] CNRS, Inst Chim Subst Nat, F-91198 Gif Sur Yvette, France
关键词
D O I
10.1021/ol036043c
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
[GRAPHICS] Two new docetaxel analogues have been prepared starting from 10-deacetylbaccatin III. Both derivatives lack the oxetane D-ring but possess the 4alpha-acetoxy group, which is important for biological activity. The influence of a more or less constrained C-ring was evaluated by adding, or not adding, a double bond in this ring. Both compounds were found to be equally less active than docetaxel in biological assays.
引用
收藏
页码:5031 / 5034
页数:4
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