12 membered Schiff base macrocyclic ligands, 6,7,14,15-tetra phenyl-1,2,3,4, 4a,8a, 9,10, 11,12, 12a,16a-dodecahydro dibenzo [b,h] [1,4,7,10] tetraazacyclododecine L1, and 14 membered Schiff base macrocyclic ligands, 6,8,15,17-tetramethyl-1,2,3,4, 4a,7,9a, 10,11,12,13,13a,16,18a-tetra decahydro dibenzo[b,i] [1, 4,8,11] cyclotetradecine tetraaza L2, 7,16-bis(2,4- dichloro benz ylidene)-6,8,15,17-tetra methyl-1,2,3,4, 4a,7,9a, 10, 11,12, 13, 13a,16,18a-tetra deca hydro dibenzo [b,i] [1,4,8,11] tetra azacyclo tetra decine L3 and 6,8,15, 17-tetramethyl-1,2,3, 4,4a,9a,10, 11,12,13,13a,18a-dodecahydro dibenzo [b,i] [1,4,8, 11] tetraazacyclo tetradecine (7,16-diylidene) bis(methanylyli dene) bis (N,N-dimethylaniline) L4 were synthesized by condensation reaction between diketone and aliphatic diamines. The metal complexes of the types, [ML1Cl2], [ML2Cl2], [ML3Cl2] and [ML4Cl2] [M= Co(II), Ni(II), Cu(II), Mn(II), Hg(II), and Fe(II)] were prepared by interaction of ligands, L1, L2, L3 and L4 with metal(II) ions. The ligands and their complexes were characterized by elemental analysis, magnetic susceptibility, conductivity measurements and IR, 1H and 13C NMR, UV–Vis spectral studies. The thermal stability of the complexes was also studied by TGA analyses. These studies show that all the complexes have octahedral arrangement around the metal ions. We used CB-Dock, a novel blind docking technique that aims to improve docking precision. With the aid of the cutting-edge docking program Autodock Vina, software online, molecular docking studies were used to evaluate the biological significance of the synthesized ligands and identify the probable and efficient binding mechanisms between the various ligands and the active site of the receptor protein. Affinity binding of both Ligand L3 and L4 to Penicillin binding protein 2x (chain B) with PDB 1PYY were much better than to Penicillin binding protein 2B (chain A) with PDB 1WAE due to the presence of hydrogen and halogen bonds. Therefore, they can be more recommended for drug design study to inhibit bacterial growth due their bioavailability. The biological activities of all compounds were evaluated like in-vitro antioxidant activity or percentage free radical scavenging effect via DPPH method against standard ascorbic acid and in vitro anticancer activity via MTT assay against colon cancer cell lines. Results of the biological activities showed that complex CuL3Cl2 exhibited the highest anti-cancer activity against colon cancer cell line i.e. 70.72±6.3 μg/ml among other copper complexes whereas compound CuL3Cl2 showed best antioxidant activity against ascorbic acid i.e. 75.07±1.96 μg/ml. While the biological activities showed that complex CuL4Cl2 exhibited the highest anti-cancer activity against colon cancer cell line i.e. 42.05±7.4 μg/ml among other copper complexes whereas compound CuL4Cl2 showed best antioxidant activity against ascorbic acid i.e. 65.47±1.37 μg/ml.
Recent reports provided evidence that epithelial to mesenchymal transition (EMT) and some matrix metalloproteinases (MMPs) contribute to the invasion and metastasis of cancer cells. This study investigated the expression pattern of some EMT markers (E-cadherin and Vimentin) and some MMPs (MMP-2 and MMP-9) in transitional cell carcinoma (TCC). Fifty five paraffin embedded biopsies were included in this study. Expression pattern of E-cadherin and Vimentin was evaluated by immunohistochemistry while cytoplasmic mRNA expression of both MMP-2 and MMP-9 were determined by in situ hybridization. The expression of all markers were significantly increased with the increase of patient's age (? 50 years), and furthermore an increase in men expression
... Show MoreCadmium has been known to be harmful to human healthy , manily Via contaminated drinking water , food supplies , tobacco and industrial pollutant . The aim of this study was to determine the toxicity of new Cadmium (II) complex ( Bis[ 5- ( P- nitrophenyl ) – ? 4 – Phenyl- 1,2,4- triazole -3- dithiocarbamatohydrazide] cadmium (II) Hydra ( 0.5) and compare it with anticancer drug cyclophosphamide ( CP) in female albino mice . This complex causes to several alterations in Enzymatic activity of Glutamate Pyruvate Transaminase (GPT) and Alkaline Phosphatase (ALP ) in three organs after the treatment of mice with different doses of a new cadmium (II) complex ( 0.09 / 0.25ml , 0.18/ 0.5ml and 0.25mg /0.7 ml /30 gm of mous
... Show MoreA new class of biologically active nanocomposites and modified polymers based on poly (vinyl alcohol) (PVA) with some organic compounds [II, IV, V and VI] were synthesized using silver nanoparticles (Ag-NPs). All compounds were synthesized using nucleophilic substitution interactions and characterized by FTIR, DSC and TGA. The biological activity of the modified polymers was evaluated against: gram (+) (staphylococcus aureus) and gram (-): (Es cherichia coli bacteria). Antimicrobial films are developed based on modified poly (vinyl alcohol) MPVA and Ag-NPs nanoparticles. The nanocomposites and modified polymers showed better antibacterial activities against Escherichia coli (Gram negative) than against Staphyloc
... Show MorePurpose: To synthesize and characterize novel Schiff base-chitosan composites and determine their antimicrobial activity. Methods: Novel Schiff-base chitosan composites were synthesized by grafting polyvinylpyrrolidone and then replacing it with different aldehydes. The resulting composites were characterized using advanced analytical techniques, including thermogravimetric analysis (TGA), x-ray diffraction (XRD) studies and Fourier transform infrared spectroscopy (FT-IR). Results: The FT-IR results revealed that the Schiff-base chitosan was successfully produced during mixing and the crystallinity change of the samples was explained by the XRD patterns. Thermogravimetric analysis (TGA) of compounds A1, A3 and A4 showed weight loss
... Show MoreThe compound azobenzen-p,p'-di(2-amine-1,3,4-thiadiazol-5-yl) (A) was formed by reacting 4,4'-(diazene-1,2-diyl)-dibenzoyl chloride with thiosemicarbazide. Ten substituted amino derivatives of azobenzen-p,p'-di(2- amine-1,3,4-thiadiazol-5-yl) were synthesized by reaction of compound (A) with formaldehyde and acetaldehyde to give Schiff base. The compound (A) reaction with sodiumcyanat and potassiumisothiocyanat gave uredo and thiouredo-1,3,4-thiadizol-5-yl. However, its reaction with benzenesulphonyl chloride and 4-methyl benzene sulphonyl chloride gave sulphonamido compounds, while its reaction with acetylchloride and benzoyl chloride gave acetamido and benzamido derivatives. Its reaction with succinic and glutaric acid gave succinamido an
... Show MorePure SnSe thin film and doped with S at different percentage (0,3,5,7)% were deposited from alloy by thermal evaporation technique on glass substrate at room temperature with 400±20nm thickness .The influences of S dopant ratio on characterization of SnSe thin film Nano crystalline was investigated by using Atomic force microscopy(AFM), X-ray diffraction (XRD), energy dispersive spectroscopy (EDS), Hall Effect measurement, UV-Vis absorption spectroscopy to study morphological, structural, electrical and optical properties respectively .The XRD showed that all the films have polycrystalline in nature with orthorhombic structure, with preferred orientation along (111)plane .These films was manufactured of very fine crystalline size in the ra
... Show MoreA novel azo dye was prepared by reacting the diazonium salt of 3-aminophenol with 8-hydroxyquinoline and subsequently used to prepare a series of Ni+2, Pd+2, Pt+4, and Cu+2 complexes. The ligand structure was characterized via1H-and 13C-nuclear magnetic resonance spectroscopy. The as-synthesized materials were characterized via Fourier-transform infrared, ultraviolet‒visible, and mass spectroscopy, as well as thermo gravimetry, differential scanning calorimetry, and elemental analysis. Conductivity, magnetic susceptibility, and the metal and chloride contents of the complexes were also determined. The ligand exhibited a trigonal geometry, whereas the Cu+2, Pd+2, Pt+4, and Ni+2 complexesexhibited tetrahedral, square planar, octahedral, and
... Show MoreAcromegaly is a condition that results from excessive growth hormone production by the anterior pituitary gland. Prolidase (PLD) is the only known human enzyme that can hydrolyze dipeptides with an amino acid at their C terminus. Reports indicate that PLD activity serves as a marker for oxidative stress in numerous disorders such as diabetes, diabetic neuropathy, chronic liver diseases, and osteoporosis. The current study aims to estimate the values of PLD, its correlation with the rest of the parameters, and ROC in acromegaly patients. A group of 61 patients with confirmed acromegaly were collected from the National Diabetic Center, Mustansyrriah University, and 60 control groups were analyzed in the same place for the par
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