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Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
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Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR, and HR-mass spectroscopy.

Results:

Compound S4 had a relatively high pharmacophore-fit score, indicating that it may have biological activity similar to the EGFR allosteric inhibitor reference, and it scored a relatively low ΔG against EGFR TK allosteric site, indicating a high likelihood of drug-receptor complex formation. Compound S4 was cytotoxic to the three cancer cell lines tested, particularly HCT-116 colorectal cancer cells, with an IC50 value comparable to Erlotinib. Compound S4 induced the intrinsic apoptotic pathway in HCT-116 cells by arresting them in the G2/M phase. All of the new derivatives, including S4, met the in silico requirements for EGFR allosteric inhibitory activity.

Conclusion:

Compound S4 is a promising EGFR tyrosine kinase allosteric inhibitor that warrants further research.

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Publication Date
Sat Dec 01 2012
Journal Name
European Journal Of Scientific Research
Evaluation of Progesterone and Estrogen Hormonal Levels in Pregnant Women with Toxoplasmosis
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In this study the prevalence of acute, sub-acute and chronic toxoplasmosis were monitored in a group of Iraqi pregnant women according to the anti-T.gondii antibodies (IgG and IgM), as well as the levels of both progesterone and estrogen hormones were measured using mini-VIDAS®technique. This study demonstrated that there was high prevalence of chronic toxoplasmosis (31.70%) when it compared with acute and sub-acute type, results also showed that the acute toxoplasmosis always related with low concentration of both progesterone and estrogen which were (5.35 ± 7.15 ng/ml) and (70.66 ± 51.08 pg/ml) respectively

Publication Date
Mon Jul 01 2024
Journal Name
Indian Journal Of Clinical Biochemistry
Evaluation of Bone Turnover Markers in Patients with Acute and Chronic Leukemia
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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Spectroscopic Characterization and Antimicrobial Activities of Some Heavy Metals Complexes of 2-hydroxy phenyl piperonalidene
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An antibacterial and antifungal piperonal-derived compound and its Rh(III), Pd(II), Pt(IV), and Cd(II) metal complexes were synthesized and characterized by spectroscopic methods, conductivity, metal analyses and magnetic moment measurements. The nature of the complexes formed in ethanolic solution was studied following the molar ratio method. From the spectral studies, octahedral geometry was suggested for rhodium (III) and platinum (IV) complexes, while a square planer structure was suggested for palladium (II) complex and a tetrahedral geometry for cadmium (II) complex. Structural geometries of these compounds were also suggested in gas phase by using hyperchem-8 program for the molecular mechanics and semi-empirical calculations.

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Publication Date
Sun Dec 31 2000
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Preparation of Tartaric Acid
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Publication Date
Sun Jan 01 2023
Journal Name
Dental Hypotheses
Assessment of the Impact of Adhesive and Wires Types on the Tensile Bond Strength of Fixed Lingual Retainers Used in Orthodontics: An In Vitro Study
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Introduction: We aimed to assess the impact of adhesive and wires types on the tensile bond strength of fixed lingual retainers. Methods: A total of 160 intact bovine teeth were collected, cleaned, stored in 25% sodium hypochlorite, and randomly assigned to two groups based on the adhesive type: a two-step adhesive and a one-step adhesive. Each group was further divided into four subgroups based on the type of lingual retainer wire, which included (A) 8-strand braided stainless steel wire, (B) three-strand titanium retainer wire, (C) stainless steel chain, and (D) fiber-reinforced retainer. A tensile bond strength test was conducted using a universal testing machine at a controlled speed of 10 mm/min. Result: The 8-strand braided stainles

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Publication Date
Thu Jul 01 2021
Journal Name
Mustansiriya Medical Journal
Evaluation of some biomarkers in diagnosis of bacterial bloodstream infection in children
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Background Bloodstream infection (BSI) is a life-threatening condition caused by the presence of microorganisms, generally caused by a range of bacteria in the blood. Objectives The aim of this study was to evaluate the possible role of procalcitonin (PCT) and C-reactive protein (CRP) as biomarkers of pediatric BSI. Methodology The study was conducted on 150 blood samples collected from the patient who admitted to Children Welfare Teaching Hospital, Medical City, Baghdad. During the period from November 2020 to March 2021, ninety blood samples from them were positive culture and 60 blood samples were negative culture (control group). The isolates were identified depending on the morphological, microscopic examination, and biochemical tests.

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Publication Date
Sun Mar 13 2011
Journal Name
Baghdad Science Journal
Use of Coliphages as an indicators of enteroviruses and faecal pollution in Water
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In spite of increasing clinical cases which caused by enteroviruses transferred by water and no documents about entericviruses in the Iraqi water standards. The use of coliphages as an indicator of enteroviruses and fecal pollution were suggested two procedures were applied . The first is Two-Step Enrichment Method and the second is Single Agar Layer Method. Both methods gives good results in Identification of coliphages through testing fifty different water samples (Tap water, Surface water and Bottled water) the study shows the presence of coliphages in fourteen samples.

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Publication Date
Tue Jun 01 2021
Journal Name
Journal Of The College Of Languages (jcl)
The Construction of a National Identification in the Novel of N. Scott Momaday House Made of Dawn
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The United States government allowed Native Americans to abandon their reservations in the 1950s and 1960s. The historical, social, and cultural backgrounds shaped the forms and themes of works by American Indian writers who urged people to refuse their culture's sense of shame. Moreover, their behavior corresponded with the restoration of individuals to their rituals after disappointment, loss of sense of life, and mental illness performed from the influence of mainstream American society. Among these writers, N. Scott Momaday and Leslie Marmon Silko participate in similar interest in portraying characters caught between indigenous beliefs and white mainstream standards.  

      The construction of

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Publication Date
Sun Dec 31 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of The Genoprotective Effect of Curcumin Against Methotrexate in Bone Marrow and Spleen Cells in Mice
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Curcumin is a yellow pigment produced from the rhizomes of the Curcuma longa plant and a primary chemo preventive component of turmeric is used as a spice and food coloring ingredient. Curcumin has a large number of pharmacological activities, such as anticancer, anti-diabetic, antioxidant, anti-infectious, and anti-inflammatory properties.Investigation of the geno-protective effect of curcumin on methotrexate induces chromosomal aberrations of spleen and bone marrow cells. In this study, 32 mice were used and divided into four groups (eight mice at each group) as follows: Group1 (negative control): Dimethyl sulfoxide was given intraperitoneally to mice every day for ten days.Group2 (positive control): Mice were received a single do

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Publication Date
Wed Sep 30 2015
Journal Name
Iraqi National Journal Of Chemistry
Evaluation of copper and zinc in Sera of Iraqi male patients with prostate cancer in Baghdad city
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Prostate cancer is an important and potentially fatal disease in humans. Both genetic and environmental risk factors are associated with increased risk of prostate cancer among Asian pop

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