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Synthesis, In Silico, and Biological Evaluation of Non‐Hydroxamate Benzoic Acid–Based Derivatives as Potential Histone Deacetylase Inhibitors (HDACi)
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ABSTRACT<p>Unregulated epigenetic modifications, including histone acetylation/deacetylation mediated by histone acetyltransferases (HATs) and histone deacetylases (HDACs), contribute to cancer progression. HDACs, often overexpressed in cancer, downregulate tumor suppressor genes, making them crucial targets for treatment. This work aimed to develop non‐hydroxamate benzoic acid–based HDAC inhibitors (HDACi) with comparable effect to the currently four FDA‐approved HDACi, which are known for their poor solubility, poor distribution, and significant side effects. All compounds were structurally verified using FTIR, <sup>1</sup>HNMR, <sup>13</sup>CNMR, and mass spectrometry. In silico analysis showed that compound <bold>A3bn</bold> (3‐chloro‐4‐((2‐(2‐(4‐hydroxybenzylidene) hydrazinyl)‐2‐oxoethyl)amino)benzoic acid) has strong binding affinity towards HDAC2, HDAC6, and HDAC8 and exhibits molecular similarity to trichostatin and SAHA (HDACi). <bold>A3bn</bold> achieved IC<sub>50</sub> values comparable to SAHA against MCF‐7 (20.3 vs. 39.2 µM) and K562 (42.0 vs. 36.1 µM) cancer cells. Western blot analysis confirmed that <bold>A3bn</bold> inhibited H3 and H4 deacetylation. Additionally, <bold>A3bn</bold> induced the extrinsic apoptotic pathway via caspase 8 activation, leading to cell death. Its enhanced activity across HDAC isoforms may result from its hydrophilic linker, facilitating zinc coordination. In conclusion, <bold>A3bn</bold> demonstrated efficacy similar to FDA‐approved HDACi and represents a promising candidate for further optimization. Future studies will focus on structural modifications to enhance potency and selectivity at lower concentrations.</p>
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Publication Date
Sat Feb 05 2022
Journal Name
Applied Nanoscience
RETRACTED ARTICLE: The impact of fear on a stage structure prey–predator system with anti-predator behavior
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A prey-predator interaction model has been suggested in which the population of a predator consists of a two-stage structure. Modified Holling's disk equation is used to describe the consumption of the prey so that it involves the additional source of food for the predator. The fear function is imposed on prey. It is supposed that the prey exhibits anti-predator behavior and may kill the adult predator due to their struggle against predation. The proposed model is investigated for existence, uniqueness, and boundedness. After determining all feasible equilibrium points, the local stability analyses are performed. In addition, global stability analyses for this model using the Lyapunov method are investigated. The chance of occurrence of loc

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Publication Date
Sat Jun 06 2026
Journal Name
Journal Of Physical Education
Using of special exercises to mtaulp speed to pass the test (150×20) for women football referees
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Publication Date
Wed Jan 10 2024
Journal Name
Journal Of Optics
Pulsed laser deposition of Pd/WO3 nanoparticles on Si nanostructure for highly sensitive room-temperature gas sensors
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Publication Date
Tue Aug 03 2021
Journal Name
Key Engineering Materials
Comparative Study of Structural Behavior for Asymmetrical Castellated (Concavely - Curved Soffit) Steel Beams with Different Strengthening Techniques
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The Asymmetrical Castellated concavely – curved soffit Steel Beams with RPC and Lacing Reinforcement improves compactness and local buckling (web and flange local buckling), vertical shear strength at gross section (web crippling and web yielding at the fillet), and net section ( net vertical shear strength proportioned between the top and bottom tees relative to their areas (Yielding)), horizontal shear strength in web post (Yielding), web post-buckling strength, overall beam flexure strength, tee Vierendeel bending moment and lateral-torsional buckling, as a result of steel section encasement. This study presents two concentrated loads test results for seven specimens Asymmetrical Castellated concavely – curved soffit Steel Be

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Publication Date
Sun Sep 07 2008
Journal Name
Baghdad Science Journal
Study the effect by CO2 laser on some optical properties of (Cd) thin film doping by Ni
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In this research study the effect of irradiation by (CW) CO2 laser on some optical properties of (Cds) doping by Ni thin films of (1)µm thickness has been prepared by heat evaporation method. (X-Ray) diffraction technique showed the prepared films before and after irradiation are ploy crystalline hexagonal structure, optical properties were include recording of absorbance spectra for prepared films in the range of (400-1000) nm wave lengths, the absorption coefficient and the energy gap were calculated before and after irradiation, finally the irradiation affected (CdS) thin films by changing its color from the Transparent yellow to dark rough yellow and decrease the value absorption coefficient also increase the value of energy gap.

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Publication Date
Mon Feb 19 2024
Journal Name
Journal Of Engineering
Predicting Biochemical Oxygen Demand at the Inlet of Al-Rustumiya Wastewater Treatment Plant Using Different Mathematical Techniques
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Water quality planning relies on Biochemical Oxygen Demand BOD. BOD testing takes five days. The Particle Swarm Optimization (PSO) is increasingly used for water resource forecasting. This work designed a PSO technique for estimating everyday BOD at Al-Rustumiya wastewater treatment facility inlet. Al-Rustumiya wastewater treatment plant provided 702 plant-scale data sets during 2012-2022. The PSO model uses the daily data of the water quality parameters, including chemical oxygen demand (COD), chloride (Cl-), suspended solid (SS), total dissolved solids (TDS), and pH, to determine how each variable affects the daily incoming BOD. PSO and multiple linear regression (MLR) findings are compared, and their performance is evaluated usin

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Publication Date
Sat Dec 01 2018
Journal Name
Political Sciences Journal
Political development on the royal regime era : A perusal according to the standards of Alexis de Tocqueville
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Abstract: The researcher aims to highlight the historical frames of political development in royal regime era (1921-1949) and study its transitions on social-political aspect for the various periods during this consistent era of Iraq history. As some elements played an important role in shaping this era’s features ,as well as 2hat succeed it, which mainly affected the political progression’s configuration, such as : political culture role, social and cultural foundation, state policy essence and the unofficial institutions remarkable role in influencing public awareness and concerning it's relation to the state ,the clan and religious institutions. The researcher employed Alexis de Tocqueville’s evaluation criteria and indi

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Publication Date
Wed Jun 30 2004
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Studying the Factors Effects on the Flowability of ZnO-CuO/γAl2O3 Catalyst Through Hopper Before Tableting Process
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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)
Cytotoxic Assay of Nigella sativa Leaf Callus Extract (Thymol) on Hep-2 Cell Line Using ELISA Assay
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Extract from cell culture of medicinal plant like Nigella sativa have been assessed for its cytotoxic properties. Thymol is likely responsible for the theraputic effects of  Nigella sativa leaf callus extract. In this short study the inhibitory effect of Nigella sativa leaf callus extract (Thymol) has been studied on Human Lorgnx Epidrmoid Carcinoma (Hep-2) cell line during different exposure period of time (24, 48 and 72 hrs.) using different concentration of the extract (1000, 500, 400, 300, 200 and 100 µg/ml). The optical density of the Hep-2 cells has been readed on 492 nm wave length. Thymol –induced cytotoxicity was (500 µg/ml) which inhibit cell growing compared to the control and this

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Publication Date
Wed Jan 01 2014
Journal Name
Aes-atema International Conference Series - Advances And Trends In Engineering Materials And Their Applications,
Back filler friction spot welding of pure commercial copper sheets to AA1050 aluminum alloy sheets (experimental study)
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