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ID: ALA1144380
Journal: Bioorg Med Chem Lett
Title: Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor.
Authors: Courtney SM, Hay PA, Buck RT, Colville CS, Phillips DJ, Scopes DI, Pollard FC, Page MJ, Bennett JM, Hircock ML, McKenzie EA, Bhaman M, Felix R, Stubberfield CR, Turner PR.
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 approximately 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.
CiteXplore: 15837312