Synthesis and biological evaluation of dianhydrohexitol integrin antagonists

被引：20

作者：

Osterkamp, F

Wehlan, H

Koert, U

Wiesner, M

Raddatz, P

Goodman, SL

机构：

[1] Humboldt Univ, Inst Chem, D-10115 Berlin, Germany

[2] Merck KGaA Preclin Res, D-64271 Darmstadt, Germany

来源：

TETRAHEDRON | 1999年 / 55卷 / 35期

关键词：

integrin antagonist; peptidomimetics; synthesis-design; 1,4 : 3,6-dianhydrohexitol;

D O I：

10.1016/S0040-4020(99)00599-2

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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 (alpha(IIb)beta(3) alpha(v)beta(3), and alpha(v)beta(5) type). Receptor binding activities in the mu mol range were observed, (C) 1999 Elsevier Science Ltd. All rights reserved.

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收藏

页码：10713 / 10734

页数：22

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