INHIBITION OF CYTIDINE DEAMINASE BY DERIVATIVES OF 1-(BETA-D-RIBOFURANOSYL)-DIHYDROPYRIMIDIN-2-ONE (ZEBULARINE)

被引：16

作者：

BARCHI, JJ ^{[1
]}

HACES, A ^{[1
]}

MARQUEZ, VE ^{[1
]}

MCCORMACK, JJ ^{[1
]}

机构：

[1] UNIV VERMONT,BURLINGTON,VT 05405

来源：

NUCLEOSIDES & NUCLEOTIDES | 1992年 / 11卷 / 10期

关键词：

D O I：

10.1080/07328319208017823

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 2'-deoxy and ara derivatives of 1-beta-(D-ribofuranosyl)-1,2-dihydropyrimidin-2-one (zebularine) were synthesized by improved routes and tested for their inhibitory properties against cytidine deaminase. It was shown that the K(i)'s of both compounds were comparable to that of the parent zebularine in inhibition studies with purified enzyme. In contrast to zebularine, 2'-deoxy and ara zebularine showed only nominal cytotoxicity against MOLT-4 and L1210 cells in vitro. A model compound for the inhibition of deoxycytidylate deaminase, 2'-deoxyzebularine 5'-monophosphate (6), was also prepared.

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页码：1781 / 1793

页数：13

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