Preferred Language
Articles
/
UvqMkJkBMF18lwyZvMsA
Synthesis, In Silico, and Biological Evaluation of Non‐Hydroxamate Benzoic Acid–Based Derivatives as Potential Histone Deacetylase Inhibitors (HDACi)
...Show More Authors
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>
Scopus Clarivate Crossref
View Publication
Publication Date
Sun Dec 31 2017
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Evaluation of Acid and Hydraulic Fracturing Treatment in Halfaya Oil Field-Sadi Formation
...Show More Authors

Sadi formation is one of the main productive formations in some of Iraqi oil fields. This formation is characterized by its low permeability values leading to low production rates that could be obtained by the natural flow.

Thus, Sadi formation in Halfaya oil field has been selected to study the success of both of "Acid fracturing" and "Hydraulic fracturing" treatments to increase the production rate in this reservoir.

   In acid fracturing, four different scenarios have been selected to verify the effect of the injected fluid acid type, concentration and their effect on the damage severity along the entire reservoir.

   The reservoir damage severity has been taken as "Shallow–Medium– Sever

... Show More
View Publication Preview PDF
Publication Date
Mon Apr 01 2013
Journal Name
International Journal Of Drug Development And Research
Therapeutic potential effects of pyridoxine and /or ascorbic acid on microalbuminuria in diabetes mellitus patient's: A randomized controlled clinical study
...Show More Authors

Objectives: This study aimed to evaluate the therapeutic potential effects of ascorbic acid or and pyridoxine on diabetic renal microalbumiuria. Methods: This was a cross-sectional study on patients with diabetes mellitus at Al-Yarmouk teaching hospital from January to December 2012, Iraq-Baghdad. Twenty one patients with diabetes mellitus (D.M), 8 IDDM and 13 IDDM were selected from, the duration of disease were ranged from 2-12 years for both type (10 females and 11males) and all enrolled patients ages were ranged from 28-65years. The concentration of total protein in urine was calculated by a biuret colorimetric assay and the urine creatinine level was measured by a modified Jaffe test. Statistical analysis: results are expressed as mean

... Show More
Scopus (4)
Scopus
Publication Date
Fri Dec 20 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences
Sulfur Derivatives of 1,2,4-Triazole: Recently Developed Compounds, Structure Activity Relationship, and Biological Activity: Review article
...Show More Authors

The term of heterocyclic chemistry focuses only on heterocyclic compounds, which consider as a percentage of organic chemistry, they equal to greater than sixty-five. These compounds are widely founded in nature and most of them are important to life. In the past few years, scientist fused on 1,2,4-triazoles and their condensed heterocyclic ring due to their medicinal significance, 1,2,4-triazole containing Sulphur atom is one of the important heterocyclic moieties due to its broad range of biological activities also their derivatives can accommodate one of the alternatives as electronic effect as exchanges of the electronic density (electron donating or withdrawing) groups ; for all what mentioned above they are consider as a core

... Show More
View Publication
Scopus (3)
Crossref (1)
Scopus Crossref
Publication Date
Mon Jul 06 2020
Journal Name
International Journal Of Research In Pharmaceutical Sciences
Obesity and Breast Cancer: Circulating Adipokines and Their Potential Diagnostic as Risk Biomarkers
...Show More Authors

Obesity and cancer are two major epidemics of this century. Obesity is related to a higher risk of many types of cancer. Studies have accessed circulating adipokines, as key-mediators in obesity and breast cancer. The study is aimed to examine the circulating levels of insulin-like growth factor-1, leptin, adiponectin, and resistin in premenopausal Iraqi women with breast cancer. The current study was performed during the period from June 2019 to December 2019 at Oncology unit/ Medical City Hospital-Baghdad. A total of 90 premenopausal women with BC/ stage II and III after 2nd dose of chemotherapy were contributed in this study as patients group. Their ages ranged from (35- 50) years in addition to 90 premenopausal healthy women wer

... Show More
View Publication
Scopus (8)
Crossref (7)
Scopus Crossref
Publication Date
Wed Aug 21 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis and characterization of new heterocyclic compounds and studying the biological activity
...Show More Authors

Scopus (1)
Scopus
Publication Date
Sun Dec 20 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, Characterization and Biological Activity of New Compounds Derived from Dapsone
...Show More Authors

New derivatives of the anti-inflammatory, leprostatic drug dapsone 4 are synthesized, characterized and biologically screened by the treating the drug dapsone with chloroacetyl chloride in the presence of base. Both amino groups are acylated to give compound 6. The symmetrical acylated product then treated with Phenol, N-Acetyl-p-aminophenol, p-Chlorophenol, m-Chlorophenol, o-Hydroxybezoic acid and m-Hydroxybezoic acid to give compounds 8(a-f). The antimicrobial activity was tested for the synthesized compounds; activates were good compared to the parent drug. All the new compounds have scanned for their biological activities toward gram ‒ve and gram +ve (M. tuberculosis, S. pneumoniae, E. coli and P. mirabilis) bacteria, the synthesized

... Show More
Publication Date
Sun Dec 06 2015
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Study the Biological Activity of New Morpholine Derivative
...Show More Authors

A new series of morpholine derivative were prepared by reacting the morpholine with ethyl chloro acetate in the presence triethylamine as an catalyst and benzene as a solvent gave the ethyl morpholin-4-ylacetate reaction with hydrazine hydrate and ethanol as a solvent gave the 2-(morpholin-4-yl)acetohydrazide gave series of Schiff base were prepared by reacting 2-(morpholin-4- yl)acetohydrazide with different aromatic aldehydes and ketons . The new series of (3-9 )were synthesis by reaction of Schiff base (10-14) with chloroacetyl chloride, triethyl amine as an catalyst and 1,4dioxane as a solvent .The chemical structures of the synthesis compound were identified by spectral methods their [ IR ,1H-NMR and 13C-NMR ].The synthesised compoun

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Wed Jan 01 2003
Journal Name
Ibn Al-haitham . J . For Pure & Appl Sci
Synthesis and characterization of new orttho - amino phenyl thio derivatives and their complexes
...Show More Authors

Two ligand ortho-amino phenyl thio benzyl (L1) and 1,3 bis (ortho - amino phenyl thio ) acetone (L2) and their complexes have been prepared and characterized . The L1 ligand is lossing phenyl group on complexcation and forming 1,2 bis (ortho - amino phenyl thio ) ethane L3 and this tetrahedrally coordinated to the metal ion ( M+2 = Ni , Cu , Cd ) and octahedrally coordinated with mercury and cobalt ions , while the ligand L2 is behave as tridentate ligand forming octahedrally around chrome metal ion . Structural , diagnosis were established by i.r , Uv- visible , conductivity elemental analysis and (mass spectra , H nmr spectra for( L1 , L2 ) .

Publication Date
Sat Nov 04 2023
Journal Name
Russian Journal Of General Chemistry
Synthesis and Characterization of Metals Complexes with Uracil and Uracil Derivatives (A Review)
...Show More Authors

Previous studies on the synthesis and characterization of metal chelates with uracil by elemental analysis, conductivity, IR, UV-Vis, NMR spectroscopy, and thermal analysis were covered in this review article. Reviewing these studies, we found that uracil can be coordinated through the electron pair on the N1, N3, O2, or O4 atoms. If the uracil was a mono-dentate ligand, it will be coordinated by one of the following atoms: N1, N3 or O2. But if the uracil was bi-dentate ligand, it will be coordinated by atoms N1 and O2, N3 and O2 or N3 and O4. However, when uracil forms complexes in the form of polymers, coordination occurs through the following atoms: N1 and N3 or N1 and O4.

Preview PDF
Scopus (52)
Crossref (51)
Scopus Clarivate Crossref
Publication Date
Sat Apr 01 2023
Journal Name
Russian Journal Of General Chemistry
Synthesis and Characterization of Metals Complexes with Uracil and Uracil Derivatives (A Review)
...Show More Authors

View Publication
Scopus (52)
Crossref (51)
Scopus Clarivate Crossref