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Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group
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Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenocarcinoma and mouse hepatoblastoma cells with low cytotoxic effect against normal human breast cells. Their binding mode to the active site of several histone deacetylases has been studied by docking and the results gave a preliminary indication that they could be successful histone deacetylase inhibitors.

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Publication Date
Sun Jul 01 2012
Journal Name
Journal Of Endodontics
Synthesis and Preliminary Evaluation of a Polyolefin-based Core for Carrier-based Root Canal Obturation
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Introduction: Carrier-based gutta-percha is an effective method of root canal obturation creating a 3-dimensional filling; however, retrieval of the plastic carrier is relatively difficult, particularly with smaller sizes. The purpose of this study was to develop composite carriers consisting of polyethylene (PE), hydroxyapatite (HA), and strontium oxide (SrO) for carrier-based root canal obturation. Methods: Composite fibers of HA, PE, and SrO were fabricated in the shape of a carrier for delivering gutta-percha (GP) using a melt-extrusion process. The fibers were characterized using infrared spectroscopy and the thermal properties determined using differential scanning calorimetry. The elastic modulus and tensile strength tests were dete

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Publication Date
Fri Jun 02 2017
Journal Name
Applied Organometallic Chemistry
A new azo‐Schiff base: Synthesis, characterization, biological activity and theoretical studies of its complexes
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A new Azo‐Schiff base ligand L was prepared by reaction of m‐hydroxy benzoic acid with (Schiff base B) of 3‐[2‐(1H–indol‐3‐yl)‐ethylimino]‐1.5‐dimethyl‐2‐phenyl‐2,3‐dihydro‐1H‐pyrazol‐4‐ylamine. This synthesized ligand was used for complexation with different metal ions like Ni(II), Co(II), Pd(II) and Pt(IV) by using a molar ratio of ligand: metal as 1:1. Resulted compounds were characterized by NMR (1H and 13C), UV–vis spectroscopy, TGA, FT‐IR, MS, elemental analysis, magnetic moment and molar conductivity studies. The activation thermodynamic parameters, such as ΔE*, ΔH*, ΔS*, ΔG*and

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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of the Possible Immuno-Protective Effect of Nigella Sativa Seed Oil on Cyclophosphamide- Induced Myelosuppression in Mice
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Myelosuppression is one of the serious adverse effects of cancer chemotherapy that lead to life threatening febrile neutropenia and considered a limiting factor for successful therapy. Cyclophosphamide a widely used anticancer drugs, induces severe bone marrow suppression by damaging hematopoietic stem cells. As cancer incidence expands globally, the demand for an effective myeloprotective therapy during cancer treatment is also increasing.Nigella sativa seed oil, a well-known plant extract that widely used for various health conditions. This study aims to evaluate the myeloprotective activity of Nigella sativa seed oil in cyclophosphamide-induced myelosuppression mice model. Myelosuppression induced by single intraperitoneal injection o

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Publication Date
Sun Sep 01 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis and Characterization of Azo Dyes Ligands Complexes with Rh (III) and La (III) and Studies Their Industrial and Bacterial Application
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1-[4-(2-Hydroxy-4, 6-dimethyl-phenylazo)-phenol]-ethanone (HL1) and 2-(4-methoxy-phenylazo)-3, 5-dimethyl-phenol (HL2) were produced by combination the diazonium salts of amines with 3, 5-dimethylphenol. The geometry of azo compounds was resolved on the basis of (C.H.N) analyses, 1H and 13CNMR, FT-IR and UV-Vis spectroscopic mechanisms. Complexes of La (III) and Rh (III) have been performed and depicted. The formation of complexes has been identified by using elemental analysis, FT-IR and UV-Vis spectroscopic process as well, conductivity molar quantifications. Nature of complexes produced have been studied obeyed mole ratio and continuous alteration ways, Beer's law followed through a concentration scope (1×10-4 - 3×10-4 M). H

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Publication Date
Sun Apr 01 2018
Journal Name
Research Journal Of Pharmaceutical, Biological And Chemical
Synthesis and characterization of azo dyes ligands complexes with Ni (II) and Cu (II) and studies their industrial and bacterial application
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1-[4-(4-Acetyl-2-hydroxy-phenylazo)-phenyl]-ethanone (L1) and 1-[3-Hydroxy-4(4-nitro-phenylazo)-phenyl]-ethanone (L2) were readied by combination the diazonium salts of amines with 3-hydroxyacetophenone. (C.H.N) analyses, infrared spectra, UV–vis electronic absorption spectra, 1H and 13CNMR spectral mechanisms are use to identified of the ligands. Complexes of Ni+2 and Cu+2 were performed as well depicted. The formation of complexes has been identified by using atomic absorption of flame, elemental analysis, infrared spectra and UV-Vis spectral process as well conductivity and magnetic quantifications. Nature of compounds produced have been studied obeyed the mole ratio and continuous contrast methods, Beer's law followed during a concent

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Publication Date
Mon Mar 01 2021
Journal Name
Journal Of Dental Sciences
Evaluation of the efficacy of lycopene gel compared with minocycline hydrochloride microspheres as an adjunct to nonsurgical periodontal treatment: A randomised clinical trial
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Publication Date
Sun Dec 01 2019
Journal Name
Saudi Medical Journal
The diagnostic power of circulating micro ribonucleic acid 34a in combination with cancer antigen 15-3 as a potential biomarker of breast cancer
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Publication Date
Mon Mar 01 2021
Journal Name
Journal Of Dental Sciences
Evaluation of the efficacy of lycopene gel compared with minocycline hydrochloride microspheres as an adjunct to nonsurgical periodontal treatment: A randomised clinical trial
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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Six-coordinate oxime-imine cobalt(III) complexes with amino acid co-ligands; synthesis and characterisation
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In this publication, several six coordinate Co(III)-complexes are reported. The reaction of 2,3-butanedione monoxime with ethylenediamine or o-phenylenediamine in mole ratios of 2:1 gave the tetradentate imine-oxime ligands diaminoethane-N,N`-bis(2-butylidine-3-onedioxime) H2L1 and o-phenylenediamine-N,N`-bis(2-butylidine-3-onedioxime), respectively. The reaction of H2L1 and H2L2 with Co(NO3)2, and the amino acid co-ligands (glycine or serine) resulted in the formation of the required complexes. Upon complex formation, the ligands behave as a neutral tetradantate species, while the amino acid co-ligand acts as a monobasic species. The mode of bonding and overall geometry of the complexes were determined through physico-chemical and spectro

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Publication Date
Sat Nov 01 2025
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
SYNTHESIS, CHARACTERIZATION, THERMAL ANALYSIS AND ANTIOXIDANT DETERMINATION FOR SOME METAL IONS COMPLEXES WITH NEW LIGAND
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The research includes the preparation of a new Schiff base(4-methyl-2-((2-phenyl hydrazineylidene)methyl)naphthalen-1-ol), which was subsequently, used to prepare a series of complexes using chlorides of Mn2+, Co2+, Cu2+, Cr3+, and Fe3+ ions. The synthesized compounds were characterized using various techniques such as elemental microanalysis (C.H.N), chloride content determination using Mohr’s method, FT-IR spectroscopy, UV-Visible, mass spectra, conductivity, DSC (Differential Scanning Calorimetry), and thermogravimetric analysis. Overall, the decay of the ligand and its metal complexes was recorded to determine their thermal stability and weight-loss profiles. The results indicated that ligand acts as a bidentate doner, coordinating wi

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