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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
Fri May 12 2023
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
SYNTHESIS, CHARACTERIZATION, ANTIMICROBIAL STUDIES, AND MOLECULAR DOCKING STUDIES OF TRANSITION METAL COMPLEXES FORMED FROM A BENZOTHIAZOLE-BASED AZO LIGAND
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The azo ligand obtained from the diazotization reaction of 2-aminobenzothiazole and 4- nitroaniline yielded a novel series of complexes with Co(II), Ni(II), Cu(II), and Zn(II) ions. The complexes were investigated using spectral techniques such as UV-Vis, FT-IR, 1H and 13C NMR spectroscopic analyses, LC-MS and atomic absorption spectrometry, electrical conductivity, and magnetic susceptibility. The molar ratio of the synthesized compounds was determined using the ligand exchange ratio, which revealed the metal-ligand ratios in the isolated complexes were 1:2. The synthesized complexes were tested for antimicrobial activity against S. aureus, E. coli, C. albicans, and C. tropicalis bacterial species. Additionally, their binding affinities we

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Publication Date
Sun Dec 04 2011
Journal Name
Baghdad Science Journal
Some Non-destructive Testing for Al metal in 0.1N of NaCl and NaOH
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In this work the corrosion behavior of Al metal was studied by using non- destructive testing (NDT), which is a noninvasive technique for determining the integrity of a material. The ultrasonic waves was used to measure the corrosion which occur by two corrosive medium (0.1N sodium chloride and 0.1N sodium hydroxide) and study the corrosion by weight-loss method and electrochemical method in addition to performance the microscopic inspection for the samples before and after the immersion in the corrosive medium. Corrosion parameters were interpreted in these media which involve corrosion potential (Ecorr) and corrosion current density (icorr). The results indicate that both

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Publication Date
Wed Dec 30 2015
Journal Name
College Of Islamic Sciences
Rooting non-violence in the Holy Quran And models of the Prophet application
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The term “non-violence” is a means of political, social, and advocacy that excludes force in reaching its objectives, and lacks infringement of the rights of non-violence. The policy of non-violence is a beautiful logic of the whole of Islamic creation, in that it is an integral part of the whole structure of Islam and it is a policy of brilliant and brilliant saying in the Almighty: `` Neither level nor good or bad, pay what is better, If that between you and him enmity as if he were intimate guardian (Suratvsalat, verse: 34. Has According to the prophet of Islam, it means that God gives to kindness (kindness) what does not give to violence (Sunan Abu Dawood, 4/255). These terms accurately communicate what is meant by violence and n

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Publication Date
Thu Nov 09 2023
Journal Name
Beirut: Al-arif Publishing House
Arabic-English Dictionary of Euphemistic and Non-literal Expressions in the Glorious Qur’an
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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Steady and unsteady flow of non-newtonian fluid in curved pipe with triangular
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This paper deals with numerical study of the flow of stable and fluid Allamstqr Aniotina in an area surrounded by a right-angled triangle has touched particularly valuable secondary flow cross section resulting from the pressure gradient In the first case was analyzed stable flow where he found that the equations of motion that describe the movement of the fluid

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Publication Date
Tue Oct 07 2025
Journal Name
Journal Of The College Of Basic Education
A comparative study between students of smokers and non-smokers in endurance antenna
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Subjects took physical fitness for health imposed on the area of research that have become an important and clear answer to the many problems resulting from the nature of dealing with modern life current actions that were needed to be hours of manual work has become accomplished by modern technology circumstance minutes, and mediated equipment And machinery. The lack of traffic rights and further burdens the intellectual and psychological pressures and the typical method of work has led to the identification of kinetic activity, thereby threatening public health in many ways stands at the forefront of these threats the problem of smoking, which causes many types of cancers, notably lung cancer. The most important reasons that led to This dr

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Publication Date
Mon Jan 01 2024
Journal Name
Cytokine
Evaluation of IL-8, nitric oxide and macrophage inhibitory factor as clinical circulatory markers in patients with cutaneous leishmaniasis, before and during sodium stibogluconate treatment
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The clinical spectrum of cutaneous leishmaniasis (CL), an intracellular parasitic pathogen, ranges from a single sore healing to chronic crusty lesions with a manifestation of treatment resistance. The complicated interaction between Leishmania bodies and the early immune response, including innate and adaptive mechanisms, determines the evolution of nodules. This study examined the levels of the chemoattractant interleukin 8 (IL-8), pro-inflammatory nitric oxide (NO), and immunoregulatory macrophage inhibitory factor (MIF) in the serum of subjects recently diagnosed with cutaneous leishmaniasis, in parallel with patients being monitored during consecutive sodium stibogluconate (Pentostam) treatment. A total of 161 serum samples of newly di

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Publication Date
Thu Oct 02 2014
Journal Name
Journal Of The Islamic University College
The image of the family in dubbed Turkish series and their potential impact on Iraqi youth
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Since the nineties of the last century, Iraqi youth have been exposed to Mexican soap operas dubbed into classical Arabic, and the stories and ideas presented by these series were almost new to all the minds of the youth at that time, a culture completely different from the culture we have of social relations, and since the number of episodes was more than Of the 100 episodes, exposure to these series has left young people confused by the addiction to all their ideas and stories. They differ from the foreign films (mostly American) that we used to watch, and they only take two hours (at most). These films contain diverse stories and may be forgotten. Memory includes events and characters in their entirety at times, and you may remember th

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Publication Date
Sat Jan 01 2011
Journal Name
Iraqi Journal Of Physics
Single Particle Level Density in a Harmonic – Oscillator Potential Well
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The purpose of this paper is to study the properties of the
partial level density ( ) l g and the total level density g ( ),
numerically obtained as a l sum of ( ) l g up to 34 max l  , for
a Harmonic – Oscillator potential well. This method applied the
quantum – mechanical phase shift technique and concentrated
on the continuum region. Also a discussion of peculiarities of
quantal calculation for single particle level density of energy –
dependent potential

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Publication Date
Mon Jan 29 2024
Journal Name
Proceedings Of The International Conference On Research Advances In Engineering And Technology - Itechcet 2022
Liquefaction potential effect in Makhool Earth dam under seismic impact
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This study is directed at investigating the liquefaction potential within earth dams using numerical modelling by two-dimensional finite element analyses method for considering the Makhool earth dam on the Tigris River in Iraq. The effect of peak ground acceleration of 0.02g, 0.04g, 0.06g, and 0.08g is viewed for a shell, and the crest is presented for all scaled earthquake duration 25 s, 50 s, 75 s, and 100 s. The current study program comprises selecting a representative history point within the Makhool earth dam as a case study. Many points were allocated at different locations within the shell and crest to observe the fluctuation in the factor of safety against liquefaction. The seepage analysis results viewed graphically for the operat

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