| Literature DB >> 16246551 |
Yong-Jiang Xu1, Hua-Quan Miao, Weitao Pan, Elizabeth C Navarro, James R Tonra, Stan Mitelman, M Margarita Camara, Dhanvanthri S Deevi, Alexander S Kiselyov, Paul Kussie, Wai C Wong, Hu Liu.
Abstract
A novel class of N-(4-{[4-(1H-benzoimidazol-2-yl)-arylamino]-methyl}-phenyl)-benzamides are described as inhibitors of the endo-beta-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 (IC(50) 0.23-0.29 microM), with the latter showing oral exposure in mice.Entities:
Mesh：
Substances：
Year: 2005 PMID： 16246551 DOI： 10.1016/j.bmcl.2005.09.070
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823