1. Academic Validation
  2. Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor

Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor

  • Bioorg Med Chem Lett. 2005 May 2;15(9):2295-9. doi: 10.1016/j.bmcl.2005.03.014.
Stephen M Courtney 1 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
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Celltech R&D Ltd, 4-10 The Quadrant, Abingdon Science Park, Abingdon, Oxfordshire OX14 4YS, UK.
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-100898
    99.62%, Heparanase Inhibitor