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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
Thu Dec 01 2022
Journal Name
Baghdad Science Journal
A Green Synthesis of Iron/Copper Nanoparticles as a Catalytic of Fenton-like Reactions for Removal of Orange G Dye
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This research paper studies the use of an environmentally and not expensive method to degrade Orange G dye (OG) from the aqueous solution, where the extract of ficus leaves has been used to fabricate the green bimetallic iron/copper nanoparticles (G-Fe/Cu-NPs). The fabricated G‑Fe/Cu-NPs were characterized utilizing scanning electron microscopy, BET, atomic force microscopy, energy dispersive spectroscopy, Fourier-transform infrared spectroscopy and zeta potential. The rounded and shaped as like spherical nanoparticles were found for G-Fe/Cu‑NPs with the size ranged 32-59 nm and the surface area was 4.452 m2/g. Then the resultant nanoparticles were utilized as a Fenton-like oxidation catalyst. The degradation efficiency of

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Publication Date
Sun Sep 06 2009
Journal Name
Baghdad Science Journal
Synthesis of several Urea plast Resins using Different Aldehydes Preparation of some Alkyde Resins and Empolyment of the prepared Resins as Additives for AZO Dyes
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Urea formaldehyde resin was prepared by using basic media by yield 95%. The Remaining of ureaplasts resin were prepared in acetic acid media by high yield. Alkyde resins were prepared by condensation polymerization by react Succinic, Maleic, Phthalic anhydrides with Ethylene glycol or Glycerol. Select samples of the prepared alkyde resins were mixed with Azo dyes in special ratio. The mixtures were used as coatings for wood, and compaised with pure dyes. The Coating that some alkyde resins showed better adhesion from using dyes alone. Preparation of wood coating by mixing ureaplast resins and alkyde resins with Azo dyes in special ratios. The coating showed better adhesion, brighter colors and better resistance to heat from Preceding coat

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Publication Date
Wed Jun 11 2025
Journal Name
Discover Oncology
The role of non-coding RNAs in the regulation of cell death pathways in melanoma
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Publication Date
Sun Apr 30 2017
Journal Name
Journal Of Engineering
Experimental Study on Heat Transfer and Friction Factor Characteristics of Single Layer Graphene Based DI-water Nanofluid in a Circular Tube under Laminar Flow and Different Heat Fluxes as Boundary Conditions
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An experimental study was performed to estimate the forced convection heat transfer performance and the pressure drop of a single layer graphene (GNPs) based DI-water nanofluid in a circular tube under a laminar flow and a uniform heat flux boundary conditions. The viscosity and thermal conductivity of nanofluid at weight concentrations of (0.1 to 1 wt%) were measured. The effects of the velocity of flow, heat flux and nanoparticle weight concentrations on the  enhancement of the heat transfer are examined. The Nusselt number of the GNPs nanofluid was enhanced as the heat flux and the velocity of flow rate  increased, and the maximum Nusselt number  ratio (Nu nanofluid/ Nu base fluid)   and thermal performance factor

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Publication Date
Sat Jan 01 2005
Journal Name
Al-khwarizmi Engineering Journal
Kinetic and Mechanism of Oxidation of Oxalic Acid by Cerium (IV)
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Kinetic and mechanism studies of the oxidation of oxalic acid by Cerium sulphate have been carried out in acid medium sulphuric acid. The uv- vis. Spectrophotometric technique was used to follow up the reaction and the selected wavelength to be followed was 320 nm. The kinetic study showed that the order of reaction is first order in Ce(IV) and fractional in oxalic acid. The effect of using different concentration of sulphuric acid on the rate of the reaction has been studied a and it was found that the rate decreased with increasing the acid concentration. Classical organic tests was used to identify the product of the oxidation reaction, the product was just bubbles of CO2.

Publication Date
Wed Dec 27 2017
Journal Name
Al-khwarizmi Engineering Journal
Kinetic and Mechanism of Oxidation of Oxalic Acid by Cerium (IV)
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Kinetic and mechanism studies of the oxidation of oxalic acid by Cerium sulphate have been carried out in acid medium sulphuric acid. The uv- vis. Spectrophotometric technique was used to follow up the reaction and the selected wavelength to be followed was 320 nm. The kinetic study showed that the order of reaction is first order in Ce(IV) and fractional in oxalic acid. The effect of using different concentration of sulphuric acid on the rate of the reaction has been studied a and it was found that the rate decreased with increasing the acid concentration. Classical organic tests was used to identify the product of the oxidation reaction, the product was just bubbles of CO2.

 

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Publication Date
Mon Sep 01 2014
Journal Name
Scholars' Press
Liquid Crystals of 2,4-Substituted-1,3-Thiazole Derivatives
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A new compounds of 2,4-substituted-1,3- thiazole containing amines [I] and [II], Schiff bases [IV] and [V], amides [VI]-[X],esters [XI] - [XIII], thiazolidinones [XIV]-[XVIII] and 1,3-oxazepines [XIX]-[XXV] were Synthesized and characterized by melting points, FTIR spectroscopy, elemental analysis, 1HNMR,13CNMR, dept135and Mass spectroscopy. The liquid crystalline properties of the synthesized compounds were verified by using hot-stage polarizing optical microscopy (POM) and differential scanning calorimeter (DSC). The compound [I] was found to be nematic textures (N). The first series of this study [II]n display only enantiotropic nematic phase when n=1-5 while the compounds with n =6-8 display two mesophasese smectic C(SmC) and nematic ph

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
Microbiological studies of a new naphthoquinone semicarbazone derivatives
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The antimicrobial activity of two naphthoquinone semicarbazone derivatives (Two newly synthesized compounds) have been studied by using tube — diluation and disc plate technique. The effect of those derivatives upon pathogenic microorganism iso-lated from specimen(urine iwounds,stool, swabs, throat ....etc) have been studied also in comparison with the antibiotics (amikacin,ampicillin, carbencillin, cephalothin, cefoxitin,clindamycin ,erythromycin,gentamycin,penicillin,tetracylin and tri-methoprim. It was shown that derivative(1) had more effective against micro organ-ism than derivative(11).

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
synthesis and characterization
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chloride or poluacrulic acid with different primary amines to mesuring==================================638one hundred three patinents with rheumatic symptoms were include in this study and their sera tested for

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Publication Date
Sun Sep 04 2011
Journal Name
Baghdad Science Journal
Chemical and Biological Study of Iraqi Kurdistan Chamomile Flower (Matricaria recutita L)
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In this study, the chamomile flowers (Matricaria recutitaL) which grow in Iraqi Kurdistan region during the seasons of (2008) are collected. The percentage of essential oil was determined by using steam distillation and the extraction of flowers performed with petroleum ether (70-80) ºC and methanol 70% using ultrasonic extraction. Total phenolic compounds were determined from methanol extracts by using Folin-Ciocalteu method. The extracts were evaluated by thin layer chromatography, ultraviolet absorption and the biological activities were evaluated through their antibacterial action against two types of bacteria using hole method. The flowers showed a composition of 0.071% ash, 0.4% essential oil, 3.2% non oily compounds, 4% oil, 1.9% mo

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