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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
Wed Jun 21 2017
Journal Name
Research Journal Of Pharmaceutical, Biological And Chemical Sciences
Synthesis and characterization of Mixed-Ligand Complexes of Oxalic Acid and Trimethoprim with Mn(II), Co(II), Ni(II), Cu(II),Zn(II), and Cr (III) Ions: and antimicrobial Activities
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Publication Date
Mon Feb 25 2019
Journal Name
Iraqi Journal Of Physics
Strain specificity in antimicrobial activity of non-thermal plasma
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Non-thermal (low-temperature) plasma may act as an alternative approach to control superficial wound and skin infections when the effectiveness of chemical agents is weak due to natural pathogen or biofilm resistance. In this paper an atmospheric pressure plasma needle jet device which generates a cold plasma jet is used to measure the effectiveness of plasma treatment against different pathogenic bacteria and to test the individual susceptibility of pathogenic bacteria to non-thermal argon plasma. It is found that, Gram-negative bacteria were more susceptible to plasma treatment than Gram-positive bacteria. For the Gram-negative bacteria Pseudomonas aeruginosa, there were no survivors among the initial 1x108C.F.U (Co

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Publication Date
Sun Jul 02 2017
Journal Name
Journal Of Educational And Psychological Researches
The rights of non-Muslims in the Islamic state
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The Islamic religion is a religion of tolerance and is pleased with worship and other legislation and the idea of peace is an authentic and profound idea related to the call for coexistence with all religions. The Prophet (PBUH) was keen to organize his relations with non-Muslims on the basis of cohabitation, On the basis of love and intolerance, God Almighty says: "If your Lord wants to make people one nation and they are still backward." Surah Hud: 118 Islam has taken care of the people and made them tolerant brothers who sympathize with their different beliefs. Which means that everyone has the right to live, believe and believe what he sees right and have the freedom to perform the acts of worship and beliefs he deems correct. The di

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Publication Date
Fri Dec 01 2023
Journal Name
Iop Conference Series: Earth And Environmental Science
Effect of Addition Different Levels of Kojic Acid and Sodium Alginate as a substitutes of conventional Antibiotic on the Characteristics of Cryopreserved Semen of Buffalo Bulls
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Abstract<p>This experiment examined the effects of adding sodium alginate and KOJIC acid as substitutes of Conventional antibiotics to soybean lecithin extender on the characteristics of cryopreserved and frozen buffalo bull semen, as well as evaluation of their additions as antibiotics that to help lowering the microbial load. Following the collection and dilution of in the soybean lecithin extender, the experimental treatments were separated into five groups, as follows: T1: (control-) without adding any antibiotics; T2: (control+) adding the conventional antibiotics Gentamicin 0.4 IU and Tylosin 0.08 IU per 100 ml; T3: adding Kojic acid at (0.06 g/L) T4: adding sodium alginate at (0.6 mg/mL)T</p> ... Show More
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Publication Date
Tue Oct 07 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of Propolis from Kurdistan region as a new resinous sealer in root canal obturation-part I biocompatibility study
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Background: Many materials were proposed as root canal obturating materials but the biocompatibility issue remains to be a critical one. Propolis has been used as a therapeutic agent since the time of Hippocrates. It is known that propolis exhibits some pharmacological activities, such as antibacterial, antiviral, antifungal and anti inflammatory activity. Materials and methods: Eighteen albino rats were used in the study and divided randomly into three groups of 6 animals for each group. Each group was scheduled to be sacrificed at different time periods, which were three days, one week and three weeks. Propolis and ZOE sealer implants of 4mm in diameter and 0.5 gm in weight were implanted in the dorsal side of the rats. At the end of the

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Publication Date
Thu Mar 20 2014
Journal Name
Molecules
Synthesis of New 2,5-Di-substituted 1,3,4-Oxadiazoles Bearing 2,6-Di-tert-butylphenol Moieties and Evaluation of Their Antioxidant Activity
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Eleven new 2,6-di-tert-butyl-4-(5-aryl-1,3,4-oxadiazol-2-yl)phenols 5a–k were synthesized by reacting aryl hydrazides with 3,5-di-tert butyl 4-hydroxybenzoic acid in the presence of phosphorus oxychloride. The resulting compounds were characterized based on their IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to test the antioxidant properties of the compounds. Compounds 5f and 5j exhibited significant free-radical scavenging ability in both assays.

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Publication Date
Thu Feb 20 2025
Journal Name
Experimental Oncology
The Potential Role of HDAC1 and HDAC3 Immunoexpression in P53 Downregulation and Tumor Aggressiveness of Colon and Rectum Carcinomas Patients
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Background. Colorectal cancer, ranking second place in global cancer mortality, arises from diverse causes. There is growing recognition of the substantial involvement of the epigenetic modifications of histones at the DNA level in the occurrence of CRC. Aim. To assess the expression of p53, HDAC1, and HDAC3 proteins in a cohort of CRC patients and to analyze potential relationship between their expression and the stages of CRC progression. Materials and Methods. The retrospective investigation was carried out on 95 paraffin-embedded CRC tissue samples. The expression of p53, HDAC1, and HDAC3 was assessed immunohistochemically. Results. Notably, the expression of the p53 protein in CRC tissue samples exhibited a prominent correlatio

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis ,spectroscopic study of Antipyryl azo 2-Naphthol and use it as new reagent for determination of Co(II) and Cu(II)
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A simple ,accurate and sensitive spectrophotometric method has been developed the determination of Cobalt(II) and Cupper (II) .The method is based on the chelation of Co(II) and Cu(II) ions with 4-(4´-pyrazolon azo) -2-Naphthol(APAN) in aqueous medium . The complexes have a maximum absorption at (513) and (506) nm and ? max 0.531×10 4 and 0.12×10 5 L.mol -1.cm -1 for Co(II) and Cu(II) respectively .The reagent and two complexes have been prepared in ethanolic solution.The stoichiometry of both complexes were found to be 1:2 (metal :legend) .The effects of various cations and anions on Co(II) and Cu(II) determination have been investigated .The stability constants and standard deviations for Co(II) and Cu(II) 0.291 x107 ,0.909X108 L.mol

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Publication Date
Sun Feb 03 2019
Journal Name
Journal Of The College Of Education For Women
Aljdhiran incision and rip and derivatives in the Qur'an: A statistical study morphological tag
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It is more beneficial science and created and the highest honor is the Koran Sciences, God has honored research in this fun science, came this research that shed the light on the radical incision, and Naughty derivatives as contained in the Koran, and illustrate the diversity of Saghma morphological, and fork them from derivatives what it entailed connotations, as well as the evacuation of cryptic in some of these verses from the biological secrets take minds newly exposed Anitrjt science under the name of scientific miracles.
The research methodology is revenue verse which included the word, and revenue lexical meaning and its meaning in the context of the Qur'an, and reflect the views of the commentators of the verse, and then the r

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Publication Date
Fri Sep 30 2022
Journal Name
Journal Of Computational Design And Engineering
CFD analysis of phase-change material-based heat storage with dimple-shaped fins: evaluation of fin configuration and distribution pattern
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Abstract<p>Phase-change materials (PCMs) have a remarkable potential for use as efficient energy storage means. However, their poor response rates during energy storage and retrieval modes require the use of heat transfer enhancers to combat these limitations. This research marks the first attempt to explore the potential of dimple-shaped fins for the enhancement of PCM thermal response in a shell-and-tube casing. Fin arrays with different dimensions and diverse distribution patterns were designed and studied to assess the effect of modifying the fin geometric parameters and distribution patterns in various spatial zones of the physical domain. The results indicate that increasing the number of </p> ... Show More
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