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  • Title: N-(4-{[4-(1H-Benzoimidazol-2-yl)-arylamino]-methyl}-phenyl)-benzamide derivatives as small molecule heparanase inhibitors.
    Author: Xu YJ, Miao HQ, Pan W, Navarro EC, Tonra JR, Mitelman S, Camara MM, Deevi DS, Kiselyov AS, Kussie P, Wong WC, Liu H.
    Journal: Bioorg Med Chem Lett; 2006 Jan 15; 16(2):404-8. PubMed ID: 16246551.
    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.
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