TRANSESTERIFICATION REACTIONS YIELD NOVEL MASKED PHOSPHATE DERIVATIVES OF THE ANTICANCER AGENT ARAC

被引:10
作者
MCGUIGAN, C [1 ]
JONES, BCNM [1 ]
RILEY, PA [1 ]
机构
[1] UNIV COLL & MIDDLESEX SCH MED,DEPT CHEM PATHOL,LONDON W1P 6DB,ENGLAND
关键词
D O I
10.1016/S0960-894X(01)81161-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Phosphate and phosphoramidate derivatives of the anti-leukemic agent araC have been prepared by a fluoride-ion mediated trans-esterification reaction. The resulting compounds, which are chiral at the phosphate centre, were tested for their ability to inhibit the incorporation of thymidine into the DNA of mammalian cells in tissue culture, and clear structure activity relationships emerged.
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页码:607 / &
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