A NOVEL ENEDIYNE PRODRUG FOR ANTIBODY-DIRECTED ENZYME PRODRUG THERAPY (ADEPT) USING ESCHERICHIA-COLI-B NITROREDUCTASE

被引：43

作者：

HAY, MP

WILSON, WR

DENNY, WA

机构：

[1] UNIV AUCKLAND,SCH MED,CANC RES LAB,AUCKLAND,NEW ZEALAND

[2] UNIV AUCKLAND,SCH MED,ONCOL SECT,AUCKLAND,NEW ZEALAND

[3] UNIV AUCKLAND,SCH MED,DEPT PATHOL,AUCKLAND,NEW ZEALAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 23期

关键词：

D O I：

10.1016/0960-894X(95)00495-F

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a novel enediyne 2, and its cytotoxicity and activation by the nitroreductase enzyme NR2 from Esherichia coli B, are described. In contrast to closely related analogues, 2 exhibits a 90-fold increase in cytoxicity against UV4 cells in the presence of the enzyme and NADH, suggesting its potential as a prodrug for Antibody-Directed Enzyme Prodrug Therapy in conjunction with E. coli nitroreductase.

引用

页码：2829 / 2834

页数：6