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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 Mar 14 2020
Journal Name
Medico-legal Update,
Fasting Versus Non-Fasting in Assessing Lipid Profile and Complete Blood Picture
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Publication Date
Tue Oct 06 2020
Journal Name
College Of Islamic Sciences
Presence and non-existence in Arabic ontological discourse are contemporary Pragmatic reading
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Mental systems in ontological discourse turned into deliberative systems, derived from the non-coordinated thought that motivated ontological discourse, as an incomplete thought, after it became close to reason; Between creation and prevention, between reasoning and creation, between submission and ambition, the result of an interconnected entity that slays one another from one another, and intersects with one another, to produce a special pattern each time, completely different from its predecessor or to provide a path for the coordination of others, which is outside the linguistic event, or part From it, signs and marks, produced to a large extent M., and united the signs; to return again in a circular and rotational movement to produc

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Publication Date
Sat Mar 30 2002
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Potential and Current Distribution in Flow Through Porous Electrochemical Reactor Working under Limiting Current Conditions
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Publication Date
Wed Jan 01 2020
Journal Name
International Journal Of Chemtech Research
Biological Assessment, Heamatological Study, and Environmental Detection of Eugenol
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Eugenol is found in essential oils of many plants. It belongs to a class of naturally occurring phenolic monoterpenoids, chemically it is an allyl chain-substituted guaiacol. A study was conducted on the compound of Eugenol, which included different studies. The first study was the determination of eugenol in body fluid, which includes serum, saliva and urine has been found the highest concentration was in urine then serum and saliva. The second study was the hematological study. Complete blood count was accomplished on the volunteers alredy administrated with eugenol contained mouthwash the analysis was accomplished before and after the mouth wash use. The result observed a slightly negative results and was not that significant, wh

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Publication Date
Tue Jan 01 2019
Journal Name
Desalination And Water Treatment
Synthesis of chitosan-iron keplerate composite as an adsorbent for removal of toxic ions from water
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Publication Date
Fri Jan 01 2021
Journal Name
Desalination And Water Treatment
Green synthesis of graphene-coated glass as novel reactive material for remediation of fluoride-contaminated groundwater
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Publication Date
Thu Dec 31 2015
Journal Name
Al-khwarizmi Engineering Journal
Effect of Acetic Acid on Electrochemical Behavior of Sealed AA2319-T3 Al-Alloys Anodized in Phosphoric Acid Electrolytes
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Abstract

      The present study investigates the effect of acetic acid on corrosion behavior and its potential of hydrothermally sealed anodized AA2319-Al-alloys. Anodizing treatment was performed in stagnant phosphoric acid electrolyte with or without addition of acetic acid. Hydrothermal sealing was carried out in boiling water for each anodized specimen. The open circuit potential of the unsealed and sealed anodized samples was examined using open circuit potential measurement for the purpose of starting in scanning polarization diagrams. The potentiostatic polarization technique measurements were performed to assess corrosion behavior and sealing quality (i.e., degree of sealing) of

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Publication Date
Fri Jun 10 2022
Journal Name
V. International Scientific Congress Of Pure, Applied And Technological Sciences
Synthesis and characterisation of new Co(II), Zn(II) and Cd(II) complexes derived from oxadiazole ligand and 1,10-phenanthroline as co-ligand
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SYNTHESIS AND CHARACTERISATION OF NEWCo(II), Zn(II) AND Cd(II) COMPLEXES DERIVED FROM OXADIAZOLE LIGAND AND 1,10-PHENANTHROLINE AS Co-LIGAND

Publication Date
Thu Mar 03 2022
Journal Name
V. International Scientific Congress Of Pure, Applied And Technological Science (minar Congress)
synthesis and characterization of new Co(II), Zn(II) and Cd(II) complexes derived from oxadiazole ligand and 1,10-phenanthroline as co-ligand
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In this work, prepared new ligand namely 5-(2,4-dichloro-phenyl)-1,3,4-oxadiazole-2-(3H)-thion, was obtained from the 2,4-dichlorobenzoyl chloride with hydrazine, after that reaxtion with CS2/KOH in methanol.

Publication Date
Sun Sep 06 2020
Journal Name
European Journal Of Dental Education
Evaluation of technology‐based learning by dental students during the pandemic outbreak of coronavirus disease 2019
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