Phosphinic acid inhibitors of matrix metalloproteinases

被引：48
|
作者：
Caldwell, CG
Sahoo, SP
Polo, SA
Eversole, RR
Lanza, TJ
Mills, SG
Niedzwiecki, LM
IzquierdoMartin, M
Chang, BC
Harrison, RK
Kuo, DW
Lin, TY
Stein, RL
Durette, PL
Hagmann, WK
机构：
[1] MERCK SHARP & DOHME RES LABS,DEPT MED CHEM,RAHWAY,NJ 07065
[2] MERCK SHARP & DOHME RES LABS,DEPT ENZYMOL,RAHWAY,NJ 07065
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 03期
关键词：
D O I：
10.1016/0960-894X(96)00023-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The matrix metalloproteinase stromelysin-1 (MMP-3) is inhibited more strongly by peptidyl phosphinic acid 7 than by its corresponding phosphonamidate and phosphonate analogs. Extending a benzyl group at P-1' to a phenylethyl group in 8 further increases the potency (K-i = 1.4 nM). Enhanced potency with an extended substituent into the P-3 region was observed.
引用
收藏
页码：323 / 328
页数：6
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