Design, synthesis, and screening of ortho-amino thiophene carboxamide derivatives on hepatocellular carcinomaas VEGFR-2Inhibitors

In this work, design, synthesis, and screening of thiophene carboxamides 4–13 and 16–23 as dual vascular endothelial growth factor receptors (VEGFRs) and mitotic inhibitors was reported. All compounds were screened against two gastrointestinal solid cancer cells, HepG-2 and HCT-116 cell lines. The most active cytotoxic derivatives 5 and 21 displayed 2.3- and 1.7-fold higher cytotoxicity than Sorafenib against HepG-2 cells. Cell cycle and apoptosis analyses for compounds 5 and 21 showed cells accumulation in the sub-G1 phase, and cell cycle arrest at G2/M phase. The apoptotic inducing activities of compounds 5 and 21were correlated to the elevation of p53, increase in Bax/Bcl-2 ratio, and increase in caspase-3/7.Compounds 5 and 21 showed potent inhibition againstVEGFR-2 (IC50 = 0.59 and 1.29 μM) and β-tubulin polymerization (73% and 86% inhibition at their IC50 values).Molecular docking was performed with VEGFR-2 and tubulin binding sites to explain the displayed inhibitory activities

Synthesis of certain 8-quinolyloxy and/or carbocyclic nitrogenous compounds for microbiological testing

Two new series as azosalicylic acid derivatives IVa-l and Va-c in addition to three series containing 8-quinolyloxy moiety Xa-i, XIIa-n and XIVa-e were synthesized for evaluation as antimicrobial compounds. Structures of the newly synthesized compounds have been deduced on the basis of elemental analysis and spectral data. Antimicrobial activity evaluation was carried using agar dilution technique; there was variability in the susceptibilities of the different organisms to the tested compounds. Staphylococcus aureus was the most resistant organism while Candida albicans was the most sensitive. Some compounds showed both antibacterial and antifungal activity, while others showed antibacterial activity with no antifungal activity and vice versa. Compound XIVe was the most active against both bacteria and fungi, while compounds Xe, XIIf, XIVa and XIVd showed a moderate activity