Synthesis and biological evaluation of dianhydrohexitol integrin antagonists

✍ Scribed by Frank Osterkamp; Hermut Wehlan; Ulrich Koert; Matthias Wiesner; Peter Raddatz; Simon L. Goodman

• Book ID: 104209562
• Publisher: Elsevier Science
• Year: 1999
• Tongue: French
• Weight: 964 KB
• Volume: 55
• Category: Article
• ISSN: 0040-4020
• DOI: 10.1016/s0040-4020(99)00599-2

✦ Synopsis

The synthesis of a series of RGD mimetics is described. All compounds have a 1.4:3.6diarthydrohexitol core, a variable linker to a guanidino group, and a serine ether to mimic the carboxylic acid. Two types of linkers were combined with 1.4:3.6-dianhydro-D-sorbitol ( I -4) and with 1,4:3,6-dianhydro-L-iditol (5). The five compounds were tested as potential integdn antagonists in a receptor binding assay (¢X,b[~3, 0Cv133, and ¢Zv[~5 type). Receptor binding activities in the pmol range were observed.