| Literature DB >> 15837312 |
Stephen M Courtney1, Philip A Hay, Richard T Buck, Claire S Colville, David J Phillips, David I C Scopes, Faye C Pollard, Martin J Page, James M Bennett, Margaret L Hircock, Edward A McKenzie, Maina Bhaman, Robert Felix, Colin R Stubberfield, Paul R Turner.
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.Entities:
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Year: 2005 PMID： 15837312 DOI： 10.1016/j.bmcl.2005.03.014
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823