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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
Mon Jan 01 2024
Journal Name
Biomed Research International
Potential Association of Maker Expression of Low‐Density Neutrophils and Their Phenotypes in Patients with Periodontitis: Control Study
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Background. Neutrophils play an important role in maintaining periodontal status in conditions of healthy homeostasis. They achieve their surveillance function by continuously migrating to the gingival sulcus and eradicating periodontal pathogens. In addition, neutrophils are considered an integral element in the pathogenesis of periodontal diseases. Among several neutrophil subsets, low‐density neutrophils (LDN) have recently received attention and are linked with cancer, immunological, inflammatory, and infectious diseases. However, the presence, phenotypes, and potential role of LDN in the pathogenesis of periodontitis have not yet been investigated. Objectives. To investiga

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Publication Date
Tue Oct 07 2025
Journal Name
Journal Of Baghdad College Of Dentistry
An in vitro evaluation of fit of the crowns fabricated by zirconium oxide-based ceramic CAD/CAM systems, before and after porcelain firing cycles and after glaze cycles
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Background: The objective of this in vitro study was to evaluate the vertical marginal fit of crowns fabricated with ZrO2 CAD/CAM, before and after porcelain firing cycles and after glaze cycles. Materials and Methods: An acrylic resin model of a left maxillary first molar was prepared and duplicated to have Nickel-Chromium master die. Ten die stone dies were sent to the CAD/CAM (Amann Girrbach) for crowns fabrication. Marginal gaps along vertical planes were measured at four indentations at the (mid mesial, mid distal, mid buccal, mid palatal) before (Time 0) and after porcelain firing cycles (Time 1) and after glaze cycles (Time 2) using a light microscope at a magnification of ×100. One way ANOVA LSD tests were performed to determine wh

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Publication Date
Tue Jan 17 2012
Journal Name
Journal Of Kerbala University
Synthesis, Characterization, of mixed ligand Complexes of (Anthranilic Acid and Nicotinamide) with Mn(II), Co(II),Ni(II), Cu(II), Zn(II) Cd(II), Hg(II) and pd(II)
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Publication Date
Wed Nov 01 2017
Journal Name
Biochemical Engineering Journal
Waste date seed oil extract as an alternative feedstock for Poly(3-hydroxybutyrate) synthesis
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Publication Date
Tue Mar 01 2016
Journal Name
Journal Of Pharmaceutical Sciences
Development and Evaluation of Biodegradable Particles Coloaded With Antigen and the Toll-Like Receptor Agonist, Pentaerythritol Lipid A, as a Cancer Vaccine
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Publication Date
Sun Oct 01 2023
Journal Name
Baghdad Science Journal
Biological peculiarities of Leucozonella retteri
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The aim of the research is to study the biology, life cycles, distribution and structure of the reproductive organ of Leucozonella retteri in natural conditions. Zoological and malacological methods are used in the work. The collection of the material was carried out according to A.A. Shileiko method. According to the results of the conducted studies, the differences between Leucozonella retteri and other species in the structure of the reproductive organ were manifested in the following. The lower part of the sperm is straight, the ovary is slightly curved. The paw pad is 8, located in 4x2 positions. The stylophore is large spherical. The vagina is cylindrical, its length is 5-6 times greater than the width. The penis is large and conve

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Publication Date
Fri Sep 01 2023
Journal Name
Al-khwarizmi Engineering Journal
High Transaction Rates Performance Evaluation for Secure E-government Based on Private Blockchain Scheme
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The implementation of technology in the provision of public services and communication to citizens, which is commonly referred to as e-government, has brought multitude of benefits, including enhanced efficiency, accessibility, and transparency. Nevertheless, this approach also presents particular security concerns, such as cyber threats, data breaches, and access control. One technology that can aid in mitigating the effects of security vulnerabilities within e-government is permissioned blockchain. This work examines the performance of the hyperledger fabric private blockchain under high transaction loads by analyzing two scenarios that involve six organizations as case studies. Several parameters, such as transaction send ra

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Publication Date
Wed Jan 01 2025
Journal Name
E3s Web Of Conferences
Assessment of radiological biological risks in samples of medicinal plants in Iraq
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The aim of this research sought to assess the background radiati on levels of medicinal plant samples in Iraq.The D, AED, and ELCRThe D values are 0.164 ± 0.006 µSv/h.The radiation dose outputs from the afore mentioned research were juxtaposed with the safety threshold of 0.247 µSv/h set by the United Nations Scientific Committee on the Effects of Atomic Radiation (UNSCEAR) in 2008 and the National Council on Radiation Pr otection and Measurements (NCRP) in 2009.The radiation exposure for all samples in this investigation is within the permissible limits.Additionally, t he AED values obtained from microsieverts per hour are (1.31 ±0.0326 mS v/y), indicating variability, with a maximum permissible limit of 2.4 mSv/y ear, as per t

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Publication Date
Mon Jan 01 2024
Journal Name
Journal Of Applied Pharmaceutical Science
The role of angiotensin converting enzyme (insertion)/(deletion) and angiotensin II type 1 receptor (A1166C) gene polymorphisms in antiproteinuric effect of ACE inhibitors in type 2 diabetic Iraqi patients
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The angiotensin converting enzyme (ACE) I\D gene polymorphism influences the blood ACE enzyme activity. Renoprotective effect of ACE inhibitors (ACEIs) varies among patients due to genetic variation, particularly in Renin-Angiotensin-Aldosterone System genes. This study investigates the genetic variations of ACE I\D and AGT1RA1166C gene polymorphisms in the antiproteinuric effect of ACEI therapy in type 2 diabetes mellitus (T2DM) patients. This is a cross-sectional study that included 76 T2DM patients who are ACEI users, divided into two groups: T2DM without diabetic kidney disease (DKD) included 31 patients, and T2DM with DKD included 45 patients. Urine samples were taken for measurement of urine albumin and creatinine, then calcul

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Publication Date
Wed Sep 16 2020
Journal Name
Al-kindy College Medical Journal
STUDY OF TINEA PEDIS IN DIABETIC VERSUS NON-DIABETIC PATIENTS
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Background : The aim of this work is to study the clinical features and causative fungi of tinea pedis in diabetic and non-diabetic patients. Result : Tinea pedis was estimated to be the second most common skin disease in the United States, after acne. Up to 15% of the U.S., population may have tinea pedis. Across Europe and East Asia, prevalence rates reach 20 %. Methods: The Complete history taking regarding: age, sex, occupation, residency, history of diabetes and diabetic profile (fasting blood sugar and post prandial).and Clinical examination of the feet Aim of the study : The aim of this work was to study the clinical features and causative fungi of tinea pedis in diabetic and non-diabetic patients Conclusion : Tinea pedis is more

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