Synthesis of highly potent and selective hetaryl ureas as integrin αvβ3-receptor antagonists

被引：18

作者：

Lange, UEW ^{[1
]}

Backfisch, G

Delzer, J

Geneste, H

Graef, C

Hornberger, W

Kling, A

Lauterbach, A

Subkowski, T

Zechel, C

机构：

[1] BASF AG, D-67056 Ludwigshafen, Germany

[2] Abbot GMBH & Co KG, D-67008 Ludwigshafen, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(02)00161-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Solid-phase synthesis and SAR of integrin alpha(v)beta(3)-receptor antagonists containing a urea moiety as non-basic guanidine mimetic are described. The most potent compounds exhibited IC50 values towards alpha(v)beta(3) in the nanomolar range and high selectivity versus related integrins like alpha(11b)beta(3). For selected examples efficacy in functional cellular assays is demonstrated. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1379 / 1382

页数：4

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