Synthesis and anticancer activity of some novel diethyl {(chromonyl/pyrazolyl) [(4-oxo-2-phenyl-quinazolin-3(4<i>H</i>)-yl)amino]methyl}phosphonates

<p>The synthesis of some novel chromonyl and pyrazolyl α-aminophosphonates containing a quinazolinone ring was carried out by applying <i>Pudovik</i> and <i>Kabachnik</i>-<i>Fields</i> reactions under solvent- and catalyst-free conditions. The anticancer activities of these compounds were evaluated against five cancer cell lines. 3-{[(3-Phenyl/1,3-diphenyl-1<i>H</i>-pyrazol-4-yl)methylidene]amino}-2-phenyl-quinazolin-4(3<i>H</i>)-ones (<b>3d,e</b>) and diethyl {[3-phenyl/1,3-diphenyl-1<i>H</i>-pyrazol-4-yl][(4-oxo-2-phenyl-quinazolin-3(4<i>H</i>) yl)amino] methyl}phosphonates (<b>4d,e</b>) displayed the potent anticancer activities against HCT116, MCF-7 and HepG2 cell lines in comparison with the standard drug.</p

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, Characterization, and Antiproliferative Activity of Cu²⁺, V(IV)O²⁺, Co²⁺, Mn²⁺, and Ni²⁺ Complexes with 3-(2-(4-Methoxyphenylcarbamothioyl)Hydrazinyl)-3-OXO-<i>N</i>-(Thiazol-2-yl)Propanamide against Human Breast Adenocarcinoma Cells

<div><p></p><p>3-(2-(4-methoxyphenylcarbamothioyl)hydrazinyl)-3-oxo-N-(thiazol-2-yl)propan-amide (H₄L) has been synthesized and its structure has been confirmed by elemental analysis, IR, mass, and ¹H and ¹³C NMR spectroscopy. This ligand has been used to synthesize complexes with Cu²⁺, V(IV)O²⁺, Co²⁺, Mn²⁺, and Ni²⁺. The structures of these complexes have been verified by elemental analyses, molar conductivities, magnetic measurements as well as UV–VIS, IR, ¹H-NMR spectroscopy. The IR spectra showed that H₄L acts as a uni-negative tetradentate or bidentate ligand. The molar conductance measurements proved that all complexes are nonelectrolytes except complexes <b>2</b> and <b>3</b>. Moreover, the metal complexes geometrical arrangements were square planar, tetrahedral, square-pyramidal, or octahedral. The structures are consistent with the IR, UV–VIS, ESR, as well as conductivity measurements. The antiproliferative activity of the synthesized complexes against human breast adenocarcinoma MCF-7 cell line showed exploited potent to moderate growth inhibitory activity, in particular complex <b>4</b> which exhibited superior potency to the reference drug cisplatin. The antitumor activity of these compounds was accompanied by significant increase in the activity of superoxide dismutase with concomitant decrease in the activities of catalase and glutathione peroxidase and reduced glutathione level. The overproduction of free radicals allowed reactive oxygen species-mediated tumor cells death.</p></div

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