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Synthesis, Antiviral and Antitumor Activity of 2- substituted-5-amidino-benzimidazoles

机译:2-取代的5-ami基-苯并咪唑类化合物的合成,抗病毒和抗肿瘤活性

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摘要

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 remarkable selectivity towards breast cancer cell line MCF-7. The most distinct and selective antiviral activity towards Coxackieviruses and Echoviruses was observed with compounds having pyridine ring at C-2. Especially interesting was fairly strong activity of the compounds 4 and 8 toward adenoviruses, which could be considered as leads against adenoviral replication.
机译:我们通过在C-2处引入各种杂环核(吡啶,N-甲基-吡咯或咪唑),制备了一组在苯并咪唑环的C-5处带有a基取代基的杂环苯并咪唑衍生物,并评估了它们的抗肿瘤和抗病毒活性。用具有咪唑啉基酰胺基取代基的化合物6和9显示出最明显的抗增殖活性。有趣的是,所有化合物均显示出对乳腺癌细胞MCF-7的显着选择性。对于在C-2具有吡啶环的化合物,观察到了对柯萨奇病毒和回声病毒的最独特和选择性的抗病毒活性。特别令人感兴趣的是化合物4和8对腺病毒的相当强的活性,这可以被认为是对抗腺病毒复制的先导。

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