Synthesis, <i>in vitro</i> and <i>in vivo</i> antitumor and antiviral activity of novel 1-substituted benzimidazole derivatives

<div><p></p><p>A novel series of 5-nitro-1<i>H</i>-benzimidazole derivatives substituted at position 1 by heterocyclic rings was synthesized. Cytotoxicity and antiviral activity of the new compounds were tested. Compound <b>3</b> was more active than doxorubicin against A-549, HCT-116 and MCF-7. However, compound <b>3</b> showed no activity against human liver carcinoma Hep G-2 cell line. Compounds <b>9</b> and <b>17b</b> (<i>E</i>) showed potency near to doxorubicin against the four cell lines. The acute toxicity of compound <b>9</b> on liver cancer induced in rats was determined <i>in vivo</i>. Interestingly, it showed restoration activity of liver function and pathology towards normal as compared to the cancer-bearing rats induced by DENA. Compounds <b>17a</b> (<i>Z</i>), <b>17b</b> (<i>E</i>) and <b>18a</b> (<i>Z</i>) were the most promising compounds for their antiviral activity against rotavirus Wa strain.</p></div