Cyclo-saligenyl-5-fluoro-2'-deoxyuridinemonophosphate (cycloSal-FdUMP) - A new prodrug approach for FdUMP

被引：13

作者：

Lorey, M

Meier, C

DeClercq, E

Balzarini, J

机构：

[1] UNIV FRANKFURT,INST ORGAN CHEM,D-60439 FRANKFURT,GERMANY

[2] KATHOLIEKE UNIV LEUVEN,REGA INST MED RES,B-3000 LOUVAIN,BELGIUM

来源：

NUCLEOSIDES & NUCLEOTIDES | 1997年 / 16卷 / 7-9期

关键词：

D O I：

10.1080/07328319708006177

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis of cycloSal-FdUMP 3a-d as a new prodrug approach for FdU 1 is described. Phosphotriesters 3 release the FdUMP 2 selectively by a controlled, chemically induced tandem reaction in hydrolysis studies. The biological activity (IC50) of cycloSal-phosphotriesters 3 was evaluated in FM3A/O cells and FM3A/TK- cells.

引用

页码：1307 / 1310

页数：4

共 6 条

[1] 5'-[4-(PIVALOYLOXY)-1,3,2-DIOXAPHOSPHORINAN-2-YL]-2'-DEOXY-5-FLUOROURIDINE - A MEMBRANE-PERMEATING PRODRUG OF 5-FLUORO-2'-DEOXYURIDYLIC ACID (FDUMP) [J].