849509-52-0Relevant articles and documents
N-(4-{[4-(1H-Benzoimidazol-2-yl)-arylamino]-methyl}-phenyl)-benzamide derivatives as small molecule heparanase inhibitors
Xu, Yong-Jiang,Miao, Hua-Quan,Pan, Weitao,Navarro, Elizabeth C.,Tonra, James R.,Mitelman, Stan,Camara, M. Margarita,Deevi, Dhanvanthri S.,Kiselyov, Alexander S.,Kussie, Paul,Wong, Wai C.,Liu, Hu
, p. 404 - 408 (2007/10/03)
A novel class of N-(4-{[4-(1H-benzoimidazol-2-yl)-arylamino]-methyl}- phenyl)-benzamides are described as inhibitors of the endo-β-glucuronidase heparanase. Among them are N-(4-{[4-(1H-benzoimidazol-2-yl)-phenylamino]-methyl} -phenyl)-3-bromo-4-methoxy-benzamide (15h), and N-(4-{[5-(1H-benzoimidazol-2-yl) -pyridin-2-ylamino]-methyl}- phenyl)-3-bromo-4-methoxy-benzamide (23) which displayed good heparanase inhibitory activity (IC50 0.23-0.29 μM), with the latter showing oral exposure in mice.