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Coordination compound (dmapH)(2)[Sn(pydc)(3)]center dot 2H(2)O (where pydc is pyridine-2,6-dicarboxylate and dmapH is 4-dimethylaminopyridine) was prepared from the reaction between the proton-transfer compound, [dmapH](2)[pydc(2-...
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Coordination compound (dmapH)(2)[Sn(pydc)(3)]center dot 2H(2)O (where pydc is pyridine-2,6-dicarboxylate and dmapH is 4-dimethylaminopyridine) was prepared from the reaction between the proton-transfer compound, [dmapH](2)[pydc(2-)] and SnCl4 center dot 5H(2)O metal salt. The structure was fully characterized by single-crystal X-ray diffraction and distorted tricapped triangular prism geometry was realized for it. The thermal behavior of the complex was investigated by TGA-DTA analyses. Then, inhibitory effect of both the complex and its ligand was tested, using oxaliplatin as a standard, under MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) method, against U251 (a human glioblastoma), H1299 (a human non-small cell lung carcinoma), beta TC (a mouse beta pancreatic), A431 (an epidermoid carcinoma) and HFF (a human foreskin fibroblast) cell lines. Potent and selective anti-proliferative effect of the complex (IC50= 1 mu M, MAE = 65.32%) and also intense decrease of mitochondrial membrane potential (MMP) was exhibited on A431 cells. Evaluation of reactive oxygen species (ROS) in cited cells confirmed that apoptotic pathway may be a possible mode for the death of cells. In order to evaluate the cellular internalization potential of the complex, A431 cells were incubated with it at IC(50)concentration. The recorded fluorescent images confirmed successful penetration of the complex.
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A ruthenium(III) complex formulated as [Ru(pyc)(3)]center dot H2O (where pyc is pyridine-2-carboxylate) was prepared through a one-pot reaction of pyridine-2,6-dicarboxylic acid and anhydrous ruthenium(III) chloride. Here, hydroth...
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A ruthenium(III) complex formulated as [Ru(pyc)(3)]center dot H2O (where pyc is pyridine-2-carboxylate) was prepared through a one-pot reaction of pyridine-2,6-dicarboxylic acid and anhydrous ruthenium(III) chloride. Here, hydrothermal conditions led to decarboxylation from pyridine-2,6-dicarboxylic acid into pyridine-2-carboxylate. The compound was identified by spectroscopic methods and its crystal structure was determined by single-crystal X-ray diffraction. The cytotoxicity of the compounds was evaluated by MTT(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) assay against three cancer cell lines containing a human melanoma (A375), a human non-small cell lung carcinoma (H1299), a human colon adenocarcinoma (HT29), and also one normal cell human foreskin fibroblast (HFF). A strong and selective inhibitory effect of the complex (IC50 = 6.50 mu M, viability inhibition = 67.12%) was exhibited toward A375 cells. The apoptosis through a mitochondrial pathway was suggested via reactive oxygen species (ROS) production and mitochondria membrane potential (MMP) collapse. The cytostatic effect of the complex in the A375 3 D spheroid model was depicted.
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Three novel Tl(III) complexes (C1), (C2) and (C3) were synthesized using the one-pot reactions of pyridine dicarboxylic acid derivatives, 2-aminobenzimidazole and/or 4-aminopyridine, and also thallium(III) nitrate trihydrate metal...
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Three novel Tl(III) complexes (C1), (C2) and (C3) were synthesized using the one-pot reactions of pyridine dicarboxylic acid derivatives, 2-aminobenzimidazole and/or 4-aminopyridine, and also thallium(III) nitrate trihydrate metal salt. The structure of all three complexes was determined by the single-crystal X-ray diffraction. C1 and C2 were realized to be isostructural with disordered square anti-prismatic geometry and for C3 arrangement of the distorted tricapped triangular prism was proposed. Cyclic voltammetry measurements on the complexes exhibited that formal potential values are more positive for C1 (E0ˊ 0.109?V) and C3 (E0ˊ 0.244?V) compared to C2 (E0ˊ –0.051?V), versus Ag/AgCl under argon. Moreover, cytotoxicity of the compounds was evaluated in vitro against two cancer cell lines including a human melanoma (A375), a human colon adenocarcinoma (HT29), and also one normal cell human foreskin fibroblast (HFF). The selective and potent cytotoxicity effect was exhibited by C1 and C3 on cancer cell lines. The apoptosis through a caspase-dependent mitochondrion pathway was confirmed by ROS production, MMP reduction, p53 activation, Bax up-regulation, and Bcl-2 down-regulation, cytochrome c release, procaspase-9, and 3 expression, for A375 cells treated to C1 and C3. According to similar cellular uptake of the complexes in A375 cell line, the generation of ROS was considered as an effective agent to justify the inhibition effect C1 and C3 on mentioned cells. Furthermore, arresting the cell cycle in the G2-M phase and inducing apoptosis were indicated by these two complexes.
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In recent years, researchers like medicinal chemists in the field of medicinal chemistry have widely utilized the 1,3,4-thiadiazole nucleus to investigate its biological and pharmacological effects. This heterocyclic structure has...
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In recent years, researchers like medicinal chemists in the field of medicinal chemistry have widely utilized the 1,3,4-thiadiazole nucleus to investigate its biological and pharmacological effects. This heterocyclic structure has demonstrated various bioactivities such as antifungal, antimicrobial, antiviral, antileishmanial, anti-inflammatory, antihypertensive, antiepileptic, and anticancer effects among others. Anticancer activity is one of its promising effect as five membered heterocyclic rings have widely been investigated by researchers in the recent years. Herein, we reviewed the chemical structures bearing 1,3,4-thiadiazole template exerting anticancer activity.
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Two new coordination complexes were synthesized using the reaction of two organic salts with gallium(III) nitrate octahydrate. The salts were prepared and used as ligand from the reaction of 2-aminobenzimidazole with pyridine-2,6-...
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Two new coordination complexes were synthesized using the reaction of two organic salts with gallium(III) nitrate octahydrate. The salts were prepared and used as ligand from the reaction of 2-aminobenzimidazole with pyridine-2,6-dicarboxylic acid and 4-hydroxypyridine-2,6-dicarboxylic acid, respectively. All compounds were identified by spectroscopic methods and their crystal structures determined by single crystal X-ray diffraction. The investigations showed that the two complexes were isostructural. Moreover, thermal analysis was carried out to study the decomposition steps of the complexes. The inhibition properties of the compounds were studied in vitro using oxaliplatin as a standard against five cell lines including a human breast cancer, a prostate cancer, a human liver hepatocellular carcinoma, a colorectal carcinoma and a human foreskin fibroblast. The anti-proliferative activity of the complexes was found to be similar in the majority of cell lines except for the prostate cancer cells. The most remarkable cytotoxicity effect of both complexes appeared on the human breast cancer cells. Determination of mitochondrial membrane potential and reactive oxygen species in this cell line suggested that apoptosis may be the main pathway for the death of the cells. (C) 2020 Elsevier B.V. All rights reserved.
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Two new coordination complexes, [pydcH(2)][Mn-2(pydc)(2)(H2O)(6)] (1) and [dmapH(2)][UO2(pydc)(2)] (2) were obtained from a compound containing dipicolinic acid and 4-dimethylaminopyridine.The complexes were characterized by X-ray...
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Two new coordination complexes, [pydcH(2)][Mn-2(pydc)(2)(H2O)(6)] (1) and [dmapH(2)][UO2(pydc)(2)] (2) were obtained from a compound containing dipicolinic acid and 4-dimethylaminopyridine.The complexes were characterized by X-ray crystallography. Electrochemical behavior of the compounds was investigated by cyclic voltammograms. Redox couples were observed at E-0' 1.625 and -0.159 V for (1) and (2) respectively, versus Ag/AgCl, under argon. After aeration, stronger interaction tendency with oxygen was exhibited for complex (1) compared to (2), within 5 min. In the next section, toxicity of each of three compounds were assayed using oxaliplatin as a standard, under MTT method, against MCF7 (a human breast cancer), HeLa (a human cervix epithelioid carcinoma) and KB (a human oral epithelial carcinoma) cell lines. Complex (1) with E-0' of about ten times (2) proved further cytotoxic potential on all three tested cancerous cell line compared to (2). The highest inhibition potential was exhibited on MCF7 cell line (IC50 = 1.00 mu M, Viability inhibition = 81.19%) for (1). Determination of mitochondrial membrane potential (MMP) and reactive oxygen species (ROS) in treated MCF7 cells with (1) confirmed a clear decrease in MMP and sharp increases in ROS generation in this cell line. (C) 2020 Elsevier Ltd. All rights reserved.
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Two new Cobalt(II) (C1) and Zinc(II) (C2) complexes were synthesized using the one-pot reaction of their metal salts with pyridine-2,6-dicarboxylic and also, amines containing 4-aminopyridine and/or 2-aminobenzimidazole, respectiv...
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Two new Cobalt(II) (C1) and Zinc(II) (C2) complexes were synthesized using the one-pot reaction of their metal salts with pyridine-2,6-dicarboxylic and also, amines containing 4-aminopyridine and/or 2-aminobenzimidazole, respectively. The structure of both compounds was determined by spectroscopic methods and single-crystal X-ray diffraction. The disordered octahedral geometry was proposed for both complexes. Cyclic voltammetry measurements on the compounds showed that C1 is a redox-active compound while significant electrochemical activity did not exhibit for C2, versus Ag/AgCl under argon. The anti-proliferative effect of the compounds was studied in vitro using oxaliplatin as a standard against three cancer cell lines including a human breast cancer (MCF7), a human colon adenocarcinoma (HT29), a human lymphocyte (HL60), as well as one normal cell line human foreskin fibroblast (HFF). The remarkable inhibition effect was indicated toward MCF7 cells by C1. Therefore, the collapse of mitochondrial membrane potential (MMP) and also the generation of reactive oxygen species (ROS) were evaluated in these cells following treatment by C1. The cytostatic effect of this complex in the MCF7 3D spheroid model was depicted.
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A zinc(II) complex formulated as (4-apyH) 2[Zn(pydc)(pydcH)](2)center dot(pydcH(2))(2)center dot 10H(2)O was prepared through a one-pot reaction of pyridine-2,6-dicarboxylic acid, 4-aminopyridine, and zinc chloride anhydrous metal...
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A zinc(II) complex formulated as (4-apyH) 2[Zn(pydc)(pydcH)](2)center dot(pydcH(2))(2)center dot 10H(2)O was prepared through a one-pot reaction of pyridine-2,6-dicarboxylic acid, 4-aminopyridine, and zinc chloride anhydrous metal salt. In all the steps, only distilled water was used as the solvent. The compound was fully characterized by single-crystal X-ray diffraction and disordered octahedral geometry was recognized for it. The cytotoxicity of the complex and its ligands was evaluated by MTT method against A375, LN229, DLD1, HT29, and HFF cell lines. The strongest anti-proliferative effect of the complex was exhibited toward HT29 (IC50 = 10 mu M, Viability inhibition = 78.23%) cells. The apoptosis was proposed as the main pathway for the death of the cells according to the product of ROS high value and reduction of MMP. The antibacterial effect of compounds was studied against two Gram-positive bacteria namely Staphylococcus aureus, and Staphylococcus epidermidis, and also three Gram-negative bacteria namely Escherichia coli, Pseudomonas aeruginosa, and Proteus vulgaris. The established antibacterial tests were including the broth microdilution method and the agar well diffusion method. S. aureus (MIC = 16 mu g/mL, IZD = 30 mm) and S. epidermidis (MIC = 32 mu g/mL, IZD = 22 mm) were considered as the most susceptible bacteria following treatment of the complex. (C) 2021 Published by Elsevier B.V.
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This paper reports the synthesis of two complexes through one-pot reactions of pyridine-2,6-dicarboxylic acid (pydcH2), phenanthroline, and 2-aminopyridine, with Gd(NO3)3.6H2O and Ce (NO3)3.6H2O metal salts. The new coordination c...
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This paper reports the synthesis of two complexes through one-pot reactions of pyridine-2,6-dicarboxylic acid (pydcH2), phenanthroline, and 2-aminopyridine, with Gd(NO3)3.6H2O and Ce (NO3)3.6H2O metal salts. The new coordination complexes C1 and C2 were identified by spectroscopic methods. The complexes were characterized by X-ray crystallography. The nature of metal-ligand interactions was studied theoretically using NBO and EDANOCV analyses. The results showed that the contribution of electrostatic interactions in both complexes is considerably larger than that of orbital. However, the contribution of orbital interactions in [CeL3]2-, is more than that in [GdL3]3- (28.8% vs. 21.8%). In following, the cytotoxic effect of synthetic complexes was investigated in vitro using oxaliplatin as a standard against three cancer cell lines including human breast cancer (MCF7), human colon adenocarcinoma (HT29), human lymphocyte (HL60) and also one normal cell, human foreskin fibroblast (HFF). The most significant inhibition activity was observed by both C1 (IC50 = 80.7 mu M, Viability inhibition = 83.41%) and C2 (IC50 = 98.3 mu M, Viability inhibition = 77.19%) toward the MCF7 cell line.
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