Synthesis, characterization, and antitumor evaluation of 4-aminoximidofurazan derivatives

<p>Reactions of 3-amino-4-aminoximidofurazan (AAOF) with Wittig–Horner reagents, trialkylphosphites, trisdialkylaminophosphines as well as the thiating Lawesson and Japanese reagents were studied. Elemental analysis and spectroscopic measurements were in good accord with the structures postulated for the new products. The antitumor activities of certain selected new compounds were screened, <i>in vitro</i>, against a panel of five (liver; HepG2; breast; MCF-7; lung; A549; colon; HCT116; and prostate PC3) human solid tumor cell lines.</p> <p></p

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