Synthesis of phased cylindrical ARC antennas arrays

5 p.International audienceThis paper describes a new approach to synthesize cylindrical antenna arrays controlled by the phase excitation, to synthesize directive lobe and multilobe patterns with steered zero. The proposed method is based on iterative minimization of a function that incorporates constraints imposed in each direction. An 8-element cylindrical antenna has been simulated and tested for various types of beam configurations

Intestinal subocclusion due to colonic lipoma: a case report

Colonic lipomas are rare benign tumors infrequently met in clinical practice. Most of them are asymptomatic making frequent their fortuitous discovery. The therapeutic approach to the fortuitous discovery of a lipoma is even less clear. The treatment depends essentially on the clinical picture, on the size of the lipoma and on its location. We report the case of a 31-year old woman, which sub-occlusive accidents events revealed a lipoma of the descending colon. The diagnosis was suspected on colonoscopy and segmental colectomy was performed. The diagnosis was confirmed by histological examination. We review the literature and discuss the clinical features, diagnosis and treatment of this uncommon disease

New derivatives of sulfonylhydrazone as potential antitumor agents: Design, synthesis and cheminformatics evaluation

Phosphoinositide 3-kinase α (PI3Kα) is a propitious target for designing anticancer drugs. A series of new N\u27-(diphenylmethylene)benzenesulfonohydrazide was synthesized and characterized using FT-IR, NMR (1H and 13C), HRMS, and elemental analysis. Target compounds exhibited an antiproliferative effect against the human colon carcinoma (HCT-116) cell line. Our cheminformatics analysis indicated that the para-tailored derivatives [p-NO2 (3) and p-CF3 (7)] have better ionization potentials based on calculated Moran autocorrelations and ionization potentials. Subsequent in vitro cell proliferation assays validated our cheminformatics results by providing experimental evidence that both derivatives 3 and 7 exhibited improved antiproliferative activities against HCT-116. Hence, our results emphasized the importance of electron-withdrawing groups and hydrogen bond-acceptors in the rational design of small-molecule chemical ligands targeting PI3Kα. These results agreed with the induced-fit docking against PI3Kα, highlighting the role of p-substituted aromatic rings in guiding the ligand-PI3Kα complex formation, by targeting a hydrophobic pocket in the ligand-binding site and forming π-stacking interactions with a nearby tryptophan residue

Design, Synthesis, and Biological Evaluation of Novel MAO-A Inhibitors Targeting Lung Cancer

Lung cancer is one of the most common causes of cancer-related deaths worldwide. Monoamine Oxidase-A (MAO-A) enzyme mediates the production of reactive oxygen species (ROS) that trigger DNA damage and oxidative injury of cells resulting in tumor initiation and progression. Available MAO-A inhibitors are used as antidepressants, however, their role as anticancer agents is still under investigation. Ligand- and structure-based drug design approaches guided the discovery and development of novel MAO-A inhibitors. A series of 1H indole-2-carboxamide derivatives was prepared and characterized using 1H-NMR, 13C-NMR, and IR. The antiproliferative effects of MAO-A inhibitors were evaluated using the cell viability assay (MTT), and MAO-A activity was evaluated using MAO-A activity assay. The presumed inhibitors significantly inhibited the growth of lung cell lines in a dose- and time dependent manner. The half maximal inhibitory concentration (IC50) values of MAO-A inhibitors (S1, S2, S4, S7, and S10) were 33.37, 146.1, 208.99, 307.7, and 147.2 µM, respectively, in A549. Glide docking against MAO-A showed that the derivatives accommodate MAO-A binding cleft and engage with key binding residues. MAO-A inhibitors provide significant and consistent evidence on MAO-A activity in lung cancer and present a potential target for the development of new chemotherapeutic agents

Facile synthesis,characterization and cytotoxicity study of new 3-(indol-2-yl) bicyclotetrazatridecahexaens

A new series of thiosemicarbazone-based indole derivatives 12-15 has been prepared by condensation reaction of indole-2-carboxamide derivatives 8-11 with thiosemicarbazide. The latter compounds underwent intracyclization in the presence of chloroacetic acid and sodium acetate to afford a set of new 3-(indol-2-yl)bicyclotetrazatridecahexaens 16-19. These newly synthesized compounds have been characterized by means of FT-IR, 1H NMR, 13C NMR, HRMS, and by elemental analyses. Cytotoxic activities of the prepared compounds along with LY294002 were evaluated in vitro against normal human skin fibroblast, human colon carcinoma (HCT116), and leukemia (K562) cell lines; results revealed that the series inhibit only HCT116 cell line. In addition, results showed that compound 18 exerts apoptosis. moderate potency in HCT116 with an IC50 value of 54 ÂľM and significantly induces apoptosis.The accepted manuscript in pdf format is listed with the files at the bottom of this page. The presentation of the authors' names and (or) special characters in the title of the manuscript may differ slightly between what is listed on this page and what is listed in the pdf file of the accepted manuscript; that in the pdf file of the accepted manuscript is what was submitted by the author

Molecular Modeling, Synthesis and Biological Evaluation of N-Phenyl-4-Hydroxy-6-Methyl-2-Quinolone-3-CarboxAmides as Anticancer Agents

The emergence of phosphatidylinositol 3-kinase (PI3Kα) in cancer development has accentuated its significance as a potential target for anticancer drug design. Twenty one derivatives of N-phenyl-4-hydroxy-6-methyl-2-quinolone-3-carboxamide were synthesized and characterized using NMR (1H and 13C) and HRMS. The derivatives displayed inhibitory activity against human epithelial colorectal adenocarcinoma (Caco-2) and human colon cancer (HCT-116) cell lines: compounds 8 (IC50 Caco-2 = 98 µM, IC50 HCT-116 = 337 µM) and 16 (IC50 Caco-2 = 13 µM, IC50 HCT-116 = 240.2 µM). Results showed that compound 16 significantly affected the gene encoding AKT, BAD, and PI3K. The induced-fit docking (IFD) studies against PI3Kα demonstrated that the scaffold accommodates the kinase domains and forms H-bonds with significant binding residues