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1-[4-(1H-Benzoimidazol-2-yl)-phenyl]-3-[4-(1H-benzoimidazol-2-yl)-phenyl]-urea derivatives as small molecule heparanase inhibitors.
Pan, Weitao; Miao, Hua-Quan; Xu, Yong-Jiang; Navarro, Elizabeth C; Tonra, James R; Corcoran, Erik; Lahiji, Armin; Kussie, Paul; Kiselyov, Alexander S; Wong, Wai C; Liu, Hu.
Bioorg Med Chem Lett ; 16(2): 409-12, 2006 Jan 15.
Article in English | MEDLINE | ID: mdl-16246560

ABSTRACT

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 (IC(50) 0.075-0.27 microM). Compound 7a showed good efficacy in a B16 metastasis model.


Subject(s)
Carbanilides/pharmacology , Enzyme Inhibitors/pharmacology , Glucuronidase/antagonists & inhibitors , Lung Neoplasms/drug therapy , Melanoma, Experimental/drug therapy , Animals , Carbanilides/chemical synthesis , Carbanilides/classification , Cell Line, Tumor , Drug Design , Drug Screening Assays, Antitumor , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/classification , In Vitro Techniques , Melanoma, Experimental/secondary , Mice , Molecular Structure , Molecular Weight , Neoplasm Metastasis/drug therapy , Structure-Activity Relationship
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