1-[4-(1H-benzoimidazol-2-yl)-phenyl]-3-[4-(1H-benzoimidazol-2-yl)-phenyl]-urea derivatives as small molecule heparanase inhibitors

被引：58
作者：
Pan, WT
Miao, HQ
Xu, YJ
Navarro, EC
Tonra, JR
Corcoran, E
Lahiji, A
Kussie, P
Kiselyov, AS
Wong, WC
Liu, H
机构：
[1] ImClone Syst Inc, Dept Prot Sci, New York, NY 10014 USA
[2] ImClone Syst Inc, Dept Chem, Brooklyn, NY 11226 USA
[3] ImClone Syst Inc, Dept Expt Therapeut, New York, NY 10014 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 02期
关键词：
heparanase inhibitor; benzimidazole; urea;
D O I：
10.1016/j.bmcl.2005.09.069
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel class of 1-[4-(1H-benzoimidazol-2-yl)-phenyl]-3-[4-(1H-benzoimidazol-2-yl)-phenyl]-ureas are described as potent inhibitors of heparanase. Among them are 1,3-bis-[4-(1H-benzoimidazol-2-yl)-phenyl]-urea (7a) and 1,3-bis-[4-(5,6-dimethyl-1H-benzoimidazol-2-yl)-phenyl]-urea (7d), which displayed good heparanase inhibitory activity (IC50 0.075-0.27 mu M). Compound 7a showed good efficacy in a B16 metastasis model. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：409 / 412
页数：4
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