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

页码：323 / 328

页数：6

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