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Synthesis, Molecular Docking Study and Cytotoxicity Evaluation of some Quinazolinone Derivatives as Nonclassical Antifolates and Potential Cytotoxic Agents
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Abstract

A series of new 4(3H)-quinazolinone derivatives (S1-S4) were synthesized and characterized   by FTIR,1HNMR and 13CNMR .Their cytotoxic activity against a set of human cancer cell lines MCF-7 (breast) and A549 (lung) was evaluated using MTT assay. To detect their selectivity toward cancer cells, the compounds were also tested against epithelial cells derived from normal human fibroblast (NHF). Methotrexate (MTX) was used as a reference for comparison . All the tested compounds exhibited toxicity against the normal cells lower than cancer cells. All the tested compounds displayed higher cytotoxicity against lung cancer cell line (A549) than MTX with the most potent one is compound S2 (IC50: 5.73 µM). Among the tested compounds, compound S1 exhibited the highest antitumor activity against MCF-7cell line (IC50: 3.38 µM) compared to MTX (IC50: 27.32 µM). The binding modes of the synthesized compounds with the target proteins (DHFR and TS) were investigated by molecular docking studies using GOLD software.

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Publication Date
Sun Jun 05 2011
Journal Name
Baghdad Science Journal
Synthesis, spectroscopic and biological studies of some metal complexes with orthoamino hydrazo benzene
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Ortho amino hydrazobenzene (L) has been prepared from the reaction of ortho amino phenyl thiol with phenyl hyrazan in mole ratio(1:1). It has been characterized by elemental analysis (C, H, N), IR, UV–Vis. The complexes of the bivalent ions (Co, Ni, Cu, Zn, Pd, Cd, Hg and Pb) and the trivalent (Cr) have been prepared and characterized too. The structural have been established by elemental analysis(C,H,N), IR , UV – Vis spectra , conductivity measurements , atomic absorption and magnetic susceptibility . The complexes showed characteristic behaviour of octahedral geometry around the metal ion and the( N,N) ligand coordinated in bidentate modeexcept with pd showed square planer. ? ,kf , ?max for the complexes were estimated too . ? for Co

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
AComparative Qualitative and Quantitative Study of Anthraquinone Derivatives in the Roots of Rheum ribes and Rheum emodi by HPLC
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High performance liquid chromatography was applied for the separation and identification of four antharquinone derivatives, aloe emodin, emodin, chrysophanol and physcion. The separation was carried out using Eurospher 100, C18 column (4.6 mm i.d. x 250 mm, 5 µm) under the following conditions: acetonitile (solvent A) and water: acetic acid (99.9: 0.1 v/v, pH 3.5)( solvent B) as a mobile phase with isocratic elution with 30% solvent B at flow rate 0.8 ml/min. The detection wavelength was set at 254 nm. The four antharquinone derivatives were isolated from the Iraqi rhubarb, Rheum ribes root by preparative TLC, their structures were identified by 1H NMR and used as standards for HPLC analysis. The percentages of alo

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Publication Date
Sat Dec 15 2018
Journal Name
Journal Of Baghdad College Of Dentistry
Immunohistochemical expression of endocan, as a marker of assessment of angiogenic potential in benign vascular lesions (hemangioma, lymphangioma and lobular capillary hemangioma) of head and neck region
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 BACKGROUND: Vascular tumors are a heterogeneous group of diseases with biological behavior ranging from a hamartomatous growth to frank malignant. The pathophysiology of lymphangioma, vascular malformation and hemangioma is interconnected, blood vessels known to be the site of origin of hamartomas, venous malformations and some neoplasms as benign, tumor-like growth of vessels (hemangiomas). Angiogenesis is the process of formation of new blood vessels from an existing structure.

Aims of study Assessment of angiogenic potential in benign vascular lesions (hemangioma, lymphangioma and lobular capillary hemangioma) of head and neck region.

 Materials and Methods: Twenty-two formalin-fixed paraffin-embedd

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Publication Date
Mon Aug 01 2016
Journal Name
Journal Of Engineering
Performance Evaluation of the Investment Projects during the Implementation Phase (Najaf province as a case study)
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The construction project is a very complicated work by its nature and requires specialized knowledge to lead it to success. The construction project is complicated socially, technically and economically in its planning, management and implementation aspects due to the fact that it has many variables and multiple stakeholders in addition to being affected by the surrounding environment. Successful projects depend on three fundamental points which are cost-time, performance and specifications. The project stakeholder's objective to achieve best specifications and the cost-time frame stipulated in the contract.

The question is, was the optimum implementation accomplished? The provision for the success of the project

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Biological Evaluation of Two New Analogues of Gonadotropin Releasing Hormone (GnRH)D-alanine8 and D-alanine
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So far synthesis of Gonadotropin Releasing Hormone (GnRH) analogues reported in the literature has clarified some aspects of structural activity of the naturally released GnRH. As a part of continuing efforts for further understanding of this relationship, the present investigation was undertaken which involved synthesis and biological evaluation of two GnRH analogues, firstly, by replacement of the amino acid L-Argenine in the 8th position at the backbone structure of the natural hormone by the amino acid D-Alanine; and secondly, by replacement of the amino acid L-Glycine in the 10th position by D-Alanine also at the backbone structure of the nature hormone, to obtain the following analogues respectively:

P

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
In Vitro Cytotoxic Study for Purified Resveratrol Extracted from Grape Skin Fruit Vitis vinifera
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This study  was  conducted  with the  aim to  extract and  purify  a  polyphenolic  compound  â€œ Resveratrol” from the skin of black grapes Vitis vinifera cultivated in Iraq. The purified resveratrol is obtained after ethanolic extraction with 80% v/v solution for fresh grape skin, followed by acid hydrolysis   with   10%   HCl   solution then   the  aglycon   moiety   was  taken  with   organic   solvent

( chloroform). Using silica gel G60 packed glass column chromatography with mobile phase benzene: methanol: acetic acid  20:4:1 a

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Publication Date
Fri Nov 25 2022
Journal Name
Baghdad Science Journal
Evaluation of Some Antioxidants and Oxidative Stress Tests in Iraqi Lung Cancer Patients
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Vitamin K-dependent protein (VKDP) contributes to the development of lung cancer. The purpose of this research was to better understanding of the role of blood matrix Gla protein (MGP), VKDPs, Malondialdehyde (MDA), Superoxide dismutase (SOD) and Vitamin K (Vit K) in Iraqi patients with lung cancer before and after the first cycle of chemotherapy. Blood samples were collected from Al amal National Hospital for cancer treatment from October 2021 to May 2022, and a total of 80 samples were collected, divided into two groups (40 patient before taking a chemotherapy and 40 patients after taking chemotherapy), ranging in age from 20 to 45 years old. The results showed that although there were highly statistically significant differences in MD

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Publication Date
Sat Sep 01 2018
Journal Name
Journal Of Pharmaceutical Sciences And Research
Evaluation of some biochemical and immunological parameters changes in Iraq male with toxoplasmosis
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A total of 33 Iraq male positive for Toxoplasmosis and Iraq male negative for Toxoplasmosis (controls) were studies to Evaluation of some biochemical and immunological parameters changes.The parameters included lipid profile such as (Cholesterol(C), Triglycerides(TG), High-Density Lipoprotein (HDL), Low-Density Lipoprotein (LDL) and very Low-Density Lipoprotein (VLDL) and complement component C3 and C4. The results revealed significant decrease in the total cholesterol, Triglycerides, LDL and non-significant in vLDL (129.96±1.63, 130.69± 2.80, 87.19±1.97, 29.24± 0.83 mg/dl respectively) and non-significant increase in HDL(24.22 ±0.62) mg/dl compared with control group(152.07± 1.63, 156.48± 6.55, 99.26 ±1.39, 31.49± 1.30 and 21.31±

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Publication Date
Mon Jul 01 2024
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Evaluation of some Biochemical and Hematological Parameters in Patients with Chronic Kidney Disease
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Background: Chronic kidney disease is a condition that results from an indefinite change in the structure and function of the kidneys. A slow, steady progression characterizes it and is irreversible.  Objectives: This study aims to evaluate the findings of certain biochemical and hematological tests in samples from Iraqi CKD patients.  Methods: This study included 90 subjects, where 70 patients with chronic kidney disease and 20 healthy individuals. Blood samples were collected from the patients during their visits to Ghazi Al-Hariri Surgical Specialties' Hospital- Medical City, Baghdad, Iraq. Age, sex and body mass index were assessed for each participant followed by renal function tests [serum blood urea, creatinine, uric acid a

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis of substituted (oxazepine, Diazepine, tetrazde) via Schiff Bases for 2- Aminobenzo Thaizole Derivatives
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This work includs synthesis of several Schiff bases by condensation of 6- methoxy – 2- amino benzothiazole with some aldehydes and ketones (2- hydroxyl benzaldehyde, 4- hydroxyl benzaldehyde, 4- N,N –dimethy amino acetophenone, benzophenone) to abtain schiff bases (1-5). These schiff bases were found to react with phthalate anhydride to give oxazepine derivatives (6-10) that were reacted with primary aromatic amines to give Diazepine derivatives (11-15). Besides, we prepared new tetrazole derivatives (16-20) from the reaction of the prepared Schiff bases with sodium azide in the prepared compounds that were characterized by physical properties, FT-IR and some of the 1H-NMR and 13C –NMR spectroscopy.

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