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2.
Sci Rep ; 10(1): 11705, 2020 Jul 16.
Artículo en Inglés | MEDLINE | ID: mdl-32678198

RESUMEN

The quaternized compounds (PzIL1-9) reacted with sodium tetrafluoroborate (NaBF4) to generate phosphazene based ionic liquids (PzILs), PzIL1a-9a. The newly synthesized ionic compounds (PzIL1a-9a) were verified using elemental CHN analyses and functional and spectroscopic (FTIR and 1H, 13C, 31P-NMR) analyses techniques. The thermal properties of PzIL1a-9a were investigated using thermogravimetric analysis (TGA). According to the initial decomposition temperature values calculated based on the TGA thermograms, PzIL7a (213 °C) was recognized to be more thermally stable than the other PzILs studied. PzIL1a-9a exhibited good solubility in the water and demonstrate a typical dielectric relaxation behavior, conductivity levels for both low and high-frequency regions. AC conductivity mechanisms and dielectric relaxation behavior of each sample are investigated by fabricating parallel plate capacitors.

3.
Sci Rep ; 10(1): 12472, 2020 07 27.
Artículo en Inglés | MEDLINE | ID: mdl-32719357

RESUMEN

Four new dicyanoargentate(I)-based complexes 1-4 were synthesized from certain metal ions with a tetradentate ligand [N, N-bis (2-hydroxyethyl) -ethylenediamine; N-bishydeten] and determined by diverse procedures (elemental, thermal, FT-IR, ESI-MS for 1-3 and, magnetic susceptibility and EPR for 1, and 2) including crystal analysis of 4. The crystal method revealed that complex 4 has a sandwich-type like polymeric chemical structure with layers formed by [Cd(N-bishydeten)2]2+ cations and [Ag(CN)2]- anions. The complexes were further characterized by fluorescence and UV spectroscopy to determine their physicochemical features. The complexes displayed a DNA binding activity within the same range as found for cisplatin, in addition to their strong stability in the presence of the physiological buffer system. The complexes were also investigated for pharmacological properties like interaction with DNA/Bovine serum albumin, anticancer and antibacterial activities. Physicochemical studies of DNA with the complexes suggested that the interaction mode between them are possibly both intercalative and groove binding types. These spectroscopic measurements also show that there may be a binding tendency between BSA and the complexes via hydrogen or Van der Waals bonds. The viability tests demonstrated that all the complexes exhibited antibacterial (1-4) and anticancer effects (2-4) toward ten diverse bacterial strains and three tumor cells (HT-29 colon adenocarcinoma, HeLa cervical cancer, and C6 glioma), respectively.


Asunto(s)
Antibacterianos/química , Antibacterianos/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Antibacterianos/síntesis química , Antineoplásicos/síntesis química , Línea Celular Tumoral , Células HT29 , Células HeLa , Humanos , Espectroscopía Infrarroja por Transformada de Fourier
4.
Life Sci ; 251: 117635, 2020 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-32272179

RESUMEN

Molecular structures containing gold, such as auranofin, have been extensively studied in the diagnosis and treatment of many diseases, including cancer treatment. The pharmacological properties of the newly synthesized unique gold-ligand structures have been reported for different cancer cell lines. However, findings on bishydeten-metal salt complexes with gold are rare. In this work, the synthesis of five novel cyanide-bridged coordination compounds having the closed formulae [Ni(bishydeten)][Au(CN)2]2 (1), [Cu(bishydeten)][Au(CN)2]2 (2), [Zn(bishydeten)2Au3(CN)4][Au2(CN)3] (3), [Cd(bishydeten)0,5]2[Au(CN)2]4.2H2O (4), and [Cd(bishydeten)2][Au(CN)2]2 (5) (where bisyhdeten = N,N-bis(2-hydroxyethyl)ethylene diamine), and their characterization by elemental, infrared, ESI-MS, X-ray (for 2) and thermic measurement methods were performed. Complexes 1 and 3 are thermally more stable than the other three complexes. For these, pharmacological adequacies were also tested. The nucleic acid and protein binding affinities of the Au (I) compounds were also estimated by spectroscopic and electrophoretic techniques. Au (I) complexes were identified as strong chemotherapeutic with mild cytotoxicity, and they demonstrated a dose-dependent inhibition on the growth of cancer cells with IC50 at 0.11 to 0.47 µM. Investigation of mechanisms of action on cells revealed that Au (I) compounds managed to inhibit cell migration and led to a decrease in cytoskeletal proteins such as CK7 and CK20. However, Au (I) compounds failed to inhibit DNA topoisomerase I. Overall, and we suggest that potent antiproliferative activity, mild cytotoxicity, good solubility, and micromolar dosage of Au (I) compounds containing bisyhdeten-metal derivatives render them the potential focus of further studies as chemotherapeutic agents.


Asunto(s)
Antineoplásicos/farmacología , Proliferación Celular/efectos de los fármacos , Cianatos/farmacología , Oro/farmacología , Neoplasias/tratamiento farmacológico , Animales , Antineoplásicos/administración & dosificación , Antineoplásicos/síntesis química , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Chlorocebus aethiops , Cianatos/administración & dosificación , Cianatos/síntesis química , Relación Dosis-Respuesta a Droga , Oro/administración & dosificación , Humanos , Concentración 50 Inhibidora , Neoplasias/patología , Solubilidad , Células Vero
5.
Eur J Med Chem ; 70: 294-307, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-24161706

RESUMEN

A number of partly (7-9) and fully (10a-12d, Scheme 1) substituted mono(4-fluorobenzyl)spiro cyclotriphosphazenes was prepared. The structures of the compounds were determined by MS, FTIR, 1D and 2D NMR techniques. The crystal structures of 9, 11b and 12b were verified by X-ray diffraction analysis. In vitro cytotoxic activity of the phosphazenes (10a-12d) against HeLa cervical cancer cell lines was evaluated. Compound 12c was found to be the most effective, as it is a cytotoxic reagent that might activate apoptosis by altering mitochondrial membrane potential. Compounds 10b, 11b and 12b showed very good activity against yeast strains Candida tropicalis and Candida albicans. BamHI and HindIII digestion results demonstrate that the compounds (10a-12a, 10b-12b, 10d-12d), and (9, 10c-12c) bind with G/G and A/A nucleotides, respectively.


Asunto(s)
Aminas/química , Antifúngicos/farmacología , Antineoplásicos/farmacología , Candida/efectos de los fármacos , Compuestos Organofosforados/farmacología , Compuestos de Espiro/química , Antifúngicos/síntesis química , Antifúngicos/química , Antineoplásicos/síntesis química , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , ADN/química , ADN/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Células HeLa , Humanos , Células MCF-7 , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Modelos Moleculares , Estructura Molecular , Compuestos Organofosforados/síntesis química , Compuestos Organofosforados/química , Plásmidos/efectos de los fármacos , Relación Estructura-Actividad
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