1H-imidazole [4,5-f][1,10] phenanthroline is a promising chemical structure for cancer treatment. Herein, we synthesized a novel 1H-imidazole [4,5-f][1,10] phenanthroline derivative named IPM714 and found it exhibited selectively colorectal cancer (CRC) cells inhibitory activities, with half maximal inhibitory concentration (IC) of 1.74 μM and 2 μM in HCT116 cells and SW480 cells, respectively. The present study is intended to explore the cytotoxicity of IPM714 in cancer cells of various types and its anticancer mechanism in vitro. Cellular functional analyses indicated IPM714 can arrest HCT116 cell cycle in S phase and induce apoptosis in HCT116 and SW480 cells. Western blot and molecular docking showed that IPM714 may suppress PI3K/AKT/mTOR pathway to inhibit cell proliferation and regulate cell cycle as well as apoptosis. This study proved IPM714 to be a promising drug in CRC therapy.
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http://dx.doi.org/10.1016/j.ejphar.2022.175120 | DOI Listing |
A nitrilotriacetic acid (NTA) complex of Cu(ii) supported on silica-coated nanosized magnetite FeO@SiO-Pr-DEA-[NTA-Cu(ii)] was prepared as a new well-defined magnetically separable nanomaterial and fully characterized IR, XRD, FESEM, TEM, TGA, DLS, BET, VSM, solid-state UV-vis spectroscopy, EDX, ICP-OES, and FESEM-EDX map analyses. Thereafter, it was successfully applied as a new easily magnetically separable and reusable heterogeneous nanocatalyst for the Buchwald-Hartwig C-N bond formation reaction in DMF at 110 °C. Using this method, various kinds of nitrogen heterocycles, such as imidazoles, 2-methyl-1-imidazole, benzimidazole, indole, and 10-phenothiazine as well as aliphatic secondary amines such as piperidine, piperazine, morpholine, dimethylamine, and diethylamine, were reacted with aryl halide compounds, and the desired products were obtained with good to excellent yields.
View Article and Find Full Text PDFJ Mol Struct
February 2023
ICAR-Central Inland Fisheries Research Institute, Barrackpore, Monirampore, Kolkata, West Bengal 700120, India.
A novel drug to treat SARS-CoV-2 infections and hydroxyl chloroquine analogue, 1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2-(furan-2-yl)-4,5-diphenyl-1-imidazole (DDFDI) compound has been synthesized in one pot reaction. The novel compound DDFDI had been characterized by FT-IR, H-NMR and C-NMR spectral techniques. The geometrical structure was optimized by density functional theory (DFT) method at B3LYP/6-31G (d, p) as the basis set.
View Article and Find Full Text PDFNeurotherapeutics
July 2020
Dept. of Neuroscience, Psychology, Drug Research and Child Health - NEUROFARBA - Pharmacology and Toxicology Section, University of Florence, Viale Gaetano Pieraccini 6, 50139, Florence, Italy.
Anti-cancer therapy based on the repeated administration of oxaliplatin is limited by the development of a disabling neuropathic syndrome with detrimental effects on the patient's quality of life. The lack of effective pharmacological approaches calls for the identification of innovative therapeutic strategies based on new targets. We focused our attention on the imidazoline I receptor (I-R) and in particular on the selective I-R agonist 2-(1-([1,1'-biphenyl]-2-yl)propan-2-yl)-4,5-dihydro-1H-imidazole) (carbophenyline).
View Article and Find Full Text PDFInorg Chem
April 2018
Key Lab of Bioinorganic and Synthetic Chemistry of Ministry of Education, School of Chemistry , Sun Yat-Sen University, Guangzhou 510275 , P. R. China.
A chiral Co(II)-based coordination polymer, [Co(pimda)(HO)] (1, Hpimda = 2-propyl-1H-imidazole-4,5-dicarboxylic acid) with 3D hyperkagomé topology is reported. Upon heating/cooling, the water molecules which are coordinated to a pair of crystallographically symmetric Co(II) ions are removed/recovered discretely in two steps, giving [Co(pimda)(HO)] (2) and [Co(pimda)(HO)] (3), which is evidenced by the reversible single-crystal-to-single-crystal (SCSC) structural transformations. As the coordination geometry of the two Co(II) ions changes from octahedron to trigonal bipyramid, obvious color change from pink for 1 to dark violet for 2 and 3 is observed.
View Article and Find Full Text PDFBioorg Chem
April 2017
Medicinal Chemistry Department, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt. Electronic address:
The synthesis, pharmacological evaluation and molecular modelling study of novel naphthalen-2-yl acetate and 1,6-dithia-4,9-diazaspiro [4.4]nonane-3,8-dione derivatives as potential anticonvulsant agents are described. The newly synthesized compounds were characterized by both analytical and spectral data.
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