Tetrahedron

Synthesis and biological evaluation of dianhydrohexitol integrin antagonists

…, U Koert, M Wiesner, P Raddatz, SL Goodman

Index: Osterkamp, Frank; Wehlan, Hermut; Koert, Ulrich; Wiesner, Matthias; Raddatz, Peter; Goodman, Simon L. Tetrahedron, 1999 , vol. 55, # 35 p. 10713 - 10734

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Citation Number: 19

Abstract

The synthesis of a series of RGD mimetics is described. All compounds have a 1, 4: 3, 6- dianhydrohexitol 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 (1– 4) and with 1, 4: 3, 6-dianhydro-L-iditol (5). The five compounds were tested as potential integrin antagonists in a receptor binding assay (αIIbβ3, αvβ3, and αvβ5 type). Receptor ...