SYNTHESIS OF A NEW CLASS OF URIDINE PHOSPHORYLASE INHIBITORS

被引:25
作者
LEVESQUE, DL
WANG, EC
WEI, DC
TZENG, CC
PANZICA, RP
NAGUIB, FNM
ELKOUNI, MH
机构
[1] UNIV RHODE ISL,DEPT CHEM,KINGSTON,RI 02881
[2] KAOHSIUNG MED COLL,SCH CHEM & PHARM,KAOHSIUNG 807,TAIWAN
[3] UNIV ALABAMA,DEPT PHARMACOL,BIRMINGHAM,AL 35294
[4] UNIV ALABAMA,CTR COMPREHENS CANC,BIRMINGHAM,AL 35294
关键词
D O I
10.1002/jhet.5570300537
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A new series of potent uridine phosphorylase inhibitors have been prepared from barbituric acid. Among them, 1-[(2-hydroxyethoxy)methyl]-5(m-benzyloxy)benzylbarbituric acid (37, BBBA) is the most promising having a K-i value of 1.1 +/- 0.2 nM with uridine phosphorylase from human liver. The new inhibitors are easily synthesized and are better inhibitors of human uridine phosphorylase than their uracil counterparts.
引用
收藏
页码:1399 / 1404
页数:6
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