599202-21-8Relevant articles and documents
2,3-Dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid derivatives: A novel class of small molecule heparanase inhibitors
Courtney, Stephen M.,Hay, Philip A.,Buck, Richard T.,Colville, Claire S.,Porter, David W.,Scopes, David I. C.,Pollard, Faye C.,Page, Martin J.,Bennett, James M.,Hircock, Margaret L.,McKenzie, Edward A.,Stubberfield, Colin R.,Turner, Paul R.
, p. 3269 - 3273 (2007/10/03)
A novel class of 2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acids are described as inhibitors of the endo-β-glucuronidase heparanase. Several of the compounds, for example, 2-[4-propylamino-5-[5-(4-chloro)phenyl-benzoxazol-2- yl]phenyl]-2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid (9c), display potent heparanase inhibitory activity (IC50 200-500nM) and have high selectivity (>100-fold) over human β-glucuronidase. They also show anti-angiogenic effects. Such compounds should serve as useful biological tools and may provide a basis for the design of novel therapeutic agents.
