کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1362831 | 981497 | 2007 | 8 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis, antiviral and antitumor activity of 2-substituted-5-amidino-benzimidazoles Synthesis, antiviral and antitumor activity of 2-substituted-5-amidino-benzimidazoles](/preview/png/1362831.png)
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.
Novel heterocyclic 2-substituted-5-amidino-benzimidazoles were prepared. Compounds having imidazolinylamidine-substituent showed reasonable antiproliferative activity, while all show noticeable selectivity toward breast cancer cells. Strong antiviral activity was obtained by pyridyl-substituted compounds toward coxsackieviruses and echoviruses. Distinct effect toward adenoviruses was also shown.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 13, 1 July 2007, Pages 4419–4426