SYNTHESIS, STRUCTURE ELUCIDATION AND BIOLOGICAL EVALUATION OF C-NORPACLITAXEL

被引:11
作者
LIANG, X [1 ]
KINGSTON, DGI [1 ]
LONG, BH [1 ]
FAIRCHILD, CA [1 ]
JOHNSTON, KA [1 ]
机构
[1] BRISTOL MYERS SQUIBB PHARMACEUT RES INST,PRINCETON,NJ 08543
基金
美国国家卫生研究院;
关键词
D O I
10.1016/0040-4039(95)01650-7
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Oxidation of 2'-TBDMS-6 alpha-hydroxy-7-epipaclitaxel (1) with lead tetraacetate furnished 2'-TBDMS-C-norpaclitaxel (2) and the C-seco compound 3. Deprotection of 2 with pyridinium hydrofluoride yielded C-norpaclitaxel (4). C-norpaclitaxel (4) is less effective at promoting the assembly of microtubules and less cytotoxic towards HCT116 cells than paclitaxel.
引用
收藏
页码:7795 / 7798
页数:4
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