Uncharged isocoumarin-based inhibitors of urokinase-type plasminogen activator.

ABSTRACT:

Background

Urokinase-type plasminogen activator (uPA) plays a major role in extracellular proteolytic events associated with tumor cell growth, migration and angiogenesis. Consequently, uPA is an attractive target for the development of small molecule active site inhibitors. Most of the recent drug development programs aimed at nonpeptidic inhibitors targeted at uPA have focused on arginino mimetics containing amidine or guanidine functional groups attached to aromatic or heterocyclic scaffolds. There is a general problem of limited bioavailability of these charged inhibitors. In the present study, uPA inhibitors were designed on an isocoumarin scaffold containing uncharged substituents.

Results

4-Chloro-3-alkoxyisocoumarins were synthesized in which the 3-alkoxy group conta

SUBMITTER: Heynekamp JJ 

PROVIDER: S-EPMC1479381 | biostudies-literature | 2006 Feb

REPOSITORIES: biostudies-literature