Synthesis and biological evaluation of C-13 amide-linked paclitaxel (Taxol) analogs

被引:33
作者
Chen, SH [1 ]
Farina, V [1 ]
Vyas, DM [1 ]
Doyle, TW [1 ]
机构
[1] BRISTOL MYERS SQUIBB PHARMACEUT RES INST,PRINCETON,NJ 08543
关键词
D O I
10.1021/jo952067o
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Several C-13 amidopaclitaxel analogs have been synthesized during the course of our structure-activity relationship study at the C-13 position. These include 4-deacetyl-13-amidopaclitaxel (4), 13-amidopaclitaxel 4-(methyl carbonate) derivatives (5a,b), and 13-amidopaclitaxel (6). None of these novel C-13 amidopaclitaxel analogs retain any activity in the tubulin polymerization assay or the in vitro cytotoxicity assay.
引用
收藏
页码:2065 / 2070
页数:6
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