Author/Authors :
Stephen M. Courtney، نويسنده , , Philip A. Hay، نويسنده , , Richard T. Buck، نويسنده , , Claire S. Colville، نويسنده , , David J. Phillips، نويسنده , , David I.C. Scopes، نويسنده , , Faye C. Pollard، نويسنده , , Martin J. Page، نويسنده , , James M. Bennett، نويسنده , , Margaret L. Hircock، نويسنده , , Edward A. McKenzie، نويسنده , , Maina Bhaman، نويسنده , , Robert Felix، نويسنده , , Colin R. Stubberfield، نويسنده , , Paul R. Turner، نويسنده ,
Abstract :
Using a furanylthiazole acetic acid as a starting point, a novel series of benzoxazol-5-yl acetic acid derivatives have been identified as heparanase inhibitors. Several compounds possess an IC50 of 200 nM against heparanase, for example, trans 2-[4-[3-(3,4-dichlorophenylamino)-3-oxo-1-propenyl]-2-fluorophenyl]benzoxazol-5-yl acetic acid (16e). Several of the compounds show anti-angiogenic properties. Improvement to the DMPK profile of compounds has provided compounds of potential use in in vivo models.
Keywords :
metastasis , ?-glucuronidase , Benzoxazole , angiogenesis , heparanase
