5-CYANO-2'-DEOXYURIDINE 5'-PHOSPHATE - POTENT COMPETITIVE INHIBITOR OF THYMIDYLATE SYNTHETASE

被引：7

作者：

CHANG, CTC

EDWARDS, MW

TORRENCE, PF

MERTES, MP

机构：

[1] UNIV KANSAS,SCH PHARM,DEPT MED CHEM,LAWRENCE,KS 66045

[2] NIAMDD,CHEM LAB,BETHESDA,MD 20014

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 09期

关键词：

D O I：

10.1021/jm00195a028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 5ʹ-phosphate (1) of the antiviral nucleoside 5-cyano-2ʹ-deoxyuridine was synthesized and evaluated for inhibition of thymidylate synthetase purified from methotrexate-resistant Lactobacillus casei. Compound 1 was a potent competitive inhibitor with a Kl of 0.55 µM. Irreversible enzyme inhibition by this compound could not be detected. © 1979, American Chemical Society. All rights reserved.

引用

页码：1137 / 1139

页数：3

共 25 条

[1] 5(ALPHA-BROMOACETYL)-2'-DEOXYURIDINE 5'-PHOSPHATE - MECHANISM BASED AFFINITY LABEL FOR THYMIDYLATE SYNTHETASE [J].