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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 Oct 07 2020
Journal Name
Indian Journal Of Forensic Medicine &amp; Toxicology
Biological Activity of Complexes of Some Amino Acid: Review
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Publication Date
Wed Oct 07 2020
Journal Name
Indian Journal Of Forensic Medicine &amp; Toxicology
Biological Activity of Complexes of Some Amino Acid: Review
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Publication Date
Thu Jan 01 2015
Journal Name
The International Journal Of Biotechnology,
LACTIC ACID AS SPACER BETWEEN POLY ACRYLIC ACID AND 4- AMINOANTIPYRINE
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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Lactic Acid Bacteria (LAB) with Probiotic Potential from Dengke Naniura
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Dengke Naniura is a traditional food from Sumatera Utara, Indonesia, that is produced through fermenting process, and this food is believed to contain high probiotics. The objective of the current research is to determine the potential of LAB as a probiotic that has been obtained from Dengke Naniura. Dengke Naniura was traditionally prepared from Cyprinus carpio. Four LABs have been successfully isolated from Dengke Naniura, such as D7DA3, D7B3, D7DBF and D7DN3. Those four LAB isolates were identified as Lactobacillus sp. This result has been confirmed by the non-spore forming bacterium, non-motile, and Gram-positive. Also, it has been supported by biochemical test, for the example Voges Proskauer, catalase test, Methyl

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Publication Date
Tue Dec 30 2008
Journal Name
Al-kindy College Medical Journal
Evaluation of the Potential Role of Serum Selenium in Diabetic Patients
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Background: The altered status of some essential trace elements observed in diabetes could have deleterious influences on the health of the diabetics. Objectives: To estimate and study the potential role of serum Selenium in type 1, type 2 diabetics and healthy subjects; and its relation with lipid profile and glycemic index. Methods: A case control designed study was carried out at the National Diabetes Center (NDC) / Al-Mustansiria University; on a total of 94 participants formed of 32 type 1 diabetics, 32 type 2 diabetics and 30 healthy control participants. Data collected about age, sex and BMI; also, blood samples examined for FPG, HbA1C, serum total cholesterol, HDL cholesterol, non-HDL cholesterol, serum triglyceride and sera were

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Publication Date
Tue Oct 31 2023
Journal Name
Malaysian Journal Of Science
SYNTHESIS, PHYSICOCHEMICAL ELUCIDATION AND BIOLOGICAL SCREENING STUDY OF NEW LIGAND DERIVED FROM 5,6-O-ISO PROPYLIDENE-L-ASCORBIC ACID AND ITS METAL(II) COMPLEXES
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A simple chemistry method approach was used to synthesise new ligand derivate from L-ascorbic acid and its complexes. All of them were water-soluble and are used quite extensively in the medical and pharmaceutical fields. This study synthesised the new ligand derivative from L-ascorbic acid-base using the following steps: A 5,6-O-isopropylidene-L-ascorbic acid was prepared by reacting dry acetone with L-ascorbic acid followed by reacting it with trichloroacetic acid to yield [chloro(carboxylic)methylidene]-5,6-O-isopropylidene-L-ascorbic acid in the second stage. In the third stage, the derivative was reacted with (methyl(6-methyl-2-pyridylmethyl)amine to create a new ligand (ONMILA). This novel ligand was identified using a number

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Publication Date
Thu Dec 28 2023
Journal Name
The Iraqi Journal Of Veterinary Medicine
Effect of Perfluorooctanoic Acid on Kidney Function in Diabetic and Non-‎‎Diabetic Male Guinea Pigs
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Perfluorooctanoic acid (PFOA) is a synthetic fluor-surfactant chemical used widely in ‎products that resist oil, heat, grease, stains, and water. It is also used in producing other ‎fluoropolymers. The main sources of exposure to PFOA are water, soil, and animal-‎origin food (meat, fish, and dairy products). The aim of this study to evaluate the renal ‎function following oral gavage of sub-lethal dose of PFOA in diabetic and non-diabetic ‎guinea pigs. The experiment run for 4 weeks, total of 40 male guinea pigs, ‎‎(Cavia porcellus), were randomly selected and grouped into four equal groups. The first ‎group (G1) served as the negative control; 2nd group (G2) alloxan induced diabetic, 3rd ‎group (G3) non-diabeti

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Publication Date
Sun Dec 27 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and evaluation of B-cyclodextrin Based Nanosponges of 5- Fluorouracil by Using Ultrasound Assisted Method
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CD-nanosponges were prepared by crosslinking B-CD with diphenylcarbonate (DPC) using ultrasound assisted technique. 5-FU was incorporated with NS by freeze drying, and the phase solubility study, complexation efficiency (CE) entrapment efficiency were performed. Also, the particle morphology was studied using SEM and AFM. The in-vitro release of 5-FU from the prepared nanosponges was carried out in 0.1N HCl.

5-FU nanosponges particle size was in the nano size. The optimum formula showed a particle size of (405.46±30) nm, with a polydispersity index (PDI) (0.328±0.002) and a negative zeta potential (-18.75±1.8). Also the drug entrapment efficiency varied with the CD: DPC molar ratio from 15.6 % to 30%. The SEM an

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Publication Date
Mon Nov 18 2024
Journal Name
Molecular Crystals And Liquid Crystals
Synthesis and liquid crystal properties of a new class of calamitic mesogens based on twin 1,3,4-thiadiazole derivatives with imine linkage
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Publication Date
Sun Aug 11 2024
Journal Name
Al-salam Journal For Medical Science
A review of recent developments in pharmaceutical chemistry on biological evolution of tetrazole derivatives
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This review sums up the developments in the biological activity of tetrazole active derivatives in recent days. Some of the deliberated derivatives of tetrazole are at present actively scientifically studied; some of them have biological activity that enables them to be studied further in the future as a drug for various biological activities. This review seeks to offer a comprehensive analysis of the efficacy and clinical advantage of biological activity for tetrazole derivatives.

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