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  • Title: Synthesis, antiviral and antitumor activity of 2-substituted-5-amidino-benzimidazoles.
    Author: Starcević K, Kralj M, Ester K, Sabol I, Grce M, Pavelić K, Karminski-Zamola G.
    Journal: Bioorg Med Chem; 2007 Jul 01; 15(13):4419-26. PubMed ID: 17482821.
    Abstract:
    We have prepared a set of heterocyclic benzimidazole derivatives bearing amidino substituents at C-5 of benzimidazole ring, by introducing various heterocyclic nuclei (pyridine, N-methyl-pyrrole or imidazole) at C-2, and evaluated their antitumor and antiviral activities. The most pronounced antiproliferative activity was shown with compounds 6 and 9, having imidazolinylamidino-substituent. Interestingly, all compounds show noticeable selectivity toward breast cancer cell line MCF-7. The most distinct and selective antiviral activity toward coxsackieviruses and echoviruses was observed with compounds having pyridine ring at C-2. Especially interesting was fairly strong activity of 4 and 8 toward adenoviruses, which could be considered as leads against adenoviral replication.
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