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Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR, and HR-mass spectroscopy.

Results:

Compound S4 had a relatively high pharmacophore-fit score, indicating that it may have biological activity similar to the EGFR allosteric inhibitor reference, and it scored a relatively low ΔG against EGFR TK allosteric site, indicating a high likelihood of drug-receptor complex formation. Compound S4 was cytotoxic to the three cancer cell lines tested, particularly HCT-116 colorectal cancer cells, with an IC50 value comparable to Erlotinib. Compound S4 induced the intrinsic apoptotic pathway in HCT-116 cells by arresting them in the G2/M phase. All of the new derivatives, including S4, met the in silico requirements for EGFR allosteric inhibitory activity.

Conclusion:

Compound S4 is a promising EGFR tyrosine kinase allosteric inhibitor that warrants further research.

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Publication Date
Tue Jan 01 2013
Journal Name
Al- Mustansiriyah J. Sci.
Synthesis and Characterization of Some Mixed Ligand Complexes of Quinaldic Acid and α-Picoline with Some Metal Salts

Some metal ions (Mn+2, Co+2, Ni+2, Cu+2, Zn+2, Cd+2 and Hg+2) complexes of quinaldic acid (QuinH) and α-picoline (α-Pic) have been synthesized and characterized on the basis of their , FTIR, (U.V-Vis) spectroscopy, conductivity measurements, magnetic susceptibility and atomic absorption. From the results obtained the following general formula has suggested for the prepared complexes [M(Quin)2( α-Pic)2].XH2O where M+2 = (Mn, Co, Ni, Cu, Zn, Cd and Hg), X = 2, X = zero for (Co+2 and Hg+2) complexes, (Quin-) = quinaldate ion, (α-Pic) = α-picoline. The results showed that the deprotonated ligand (QuinH) by using (KOH) coordinated to metal ions as bidentate ligand through the oxygen atom of the carboxylate group (-COO-) and the nitrogen ato

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Publication Date
Fri Jun 29 2018
Journal Name
Journal Of The College Of Education For Women
Stream of Consciousness Technique: Psychological Perspectives and Use in Modern Novel

Stream of Consciousness technique has a great impact on writing literary texts in the modern age. This technique was broadly used in the late of nineteen century as a result of thedecay of plot, especially in novel writing. Novelists began to use stream of consciousness technique as a new phenomenon, because it goes deeper into the human mind and soul through involving it in writing. Modern novel has changed after Victorian age from the traditional novel that considers themes of religion, culture, social matters, etc.  to be a group of irregular events and thoughts interrogate or reveal the inner feeling of  readers.

This study simplifies stream of consciousness technique through clarifying the three levels of conscious

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Publication Date
Wed May 10 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Turbidimetric Method for Measuring of Antibacterial Effect of 2-Methyl-4-(3,4 dihydroxy Phenyl)-Thiazole on the Growth Activity of Escherichia Coli and Pseudomonas Aeruginosa

Thiazoles are heterocyclic nitrogenous compounds, which were given a great attention due to their antibacterial effect, antihypertensive, stimulating glucose absorption (like antibiotics), acts as cytoprotective agent. The present work is conducted to evaluate the degree of antibacterial activity on the growth activity of Escherichia Coli (E.Coli) and Pseudomonas aeruginosa (P. aeruginosa) by incubation with 2-methyl-4-(3,4 dihydroxy phenyl)-Thiazole compound (MDHPT). Optical density (O.B) was measured by turbidmetric method, any increase in O.D would represent the increase in the bacterial growth .The results showed that there was a 75.7 % inhibition when using 190.4 g/ml (MDHPT) solution and 64.3% was obtained when using concentr

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Publication Date
Mon Feb 24 2025
Journal Name
Journal Of Baghdad College Of Dentistry
An In Vitro Evaluation of the Effectiveness of Gotu Kola (Centella asiatica) on Inhibiting the Growth of Selected Microorganismsin Human Saliva

Background: Gotu Kola (Centella asiatica) has been used as a traditional medicine for many years to cure different kinds of diseases. Studies have been reported that Gotu Kola extracts might be used as a cure for oral diseases such as periodontal disease. In the present study, Gotu Kola leaves extracted with water will be used to evaluate its effect on some microorganisms living in the human saliva using minimum inhibitory concentration (MIC) method. Material and Method:Gotu Kola fresh leaves extract have been used with water as a solvent, a rotary evaporator was used to separate the solvent from the extract. The following microorganisms: Streptococci, Lactobacilli, and Staphylococcus aureus have been isolated fromthe Saliva of ten voluntee

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Publication Date
Wed Jul 01 2015
Journal Name
Al–bahith Al–a'alami
The Role of the Social Networking Site (Facebook) in the Adjustment of Youth Trends / Community Issues and Problems

Recent technological developments in the mass media a major paradigm shift in important segments of society, particularly among young people in particular social networking sites including (Facebook) .
it was able to link the sprawling parts of the world and paved the way for all the communities of convergence and exchange views, ideas and desires as provided by their ability to communicate through the use of video clips,pictures,share files, chat, communicate and direct interaction between the audience for this the means. Wondered problem Find the role that can be played using the university youth to the social networking site (Facebook ) to modify their attitudes or their interest in Iraqi society issues, With focused research objec

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Crossref
Publication Date
Thu Jan 26 2006
Journal Name
Acta Crystallographica Section E
(OC-6-13)-Bis[5-bromo-2-(4-bromo­phenyl­diazenyl)phen­yl]dicarbonyl­ruthenium(II) with mutually transN-donor atoms

The title compound, [Ru(C12H7Br2N2)2(CO)2], possesses a distorted octa­hedral environment about the Ru atom, with two cyclo­metallated 4,4′-dibromo­azobenzene ligands and two mutually cis carbonyl ligands. The donor atoms are arranged such that the N atoms are mutually trans and the aryl C atoms are trans to carbonyl ligands.

Publication Date
Sun May 30 2021
Journal Name
Iraqi Journal Of Science
In Vivo and In Vitro Study of the Genetic Effects of Cabergoline Drug

This study aimed to stand on genetic effects important of cabergoline drug. This toxic effect was evaluated for three different doses (0.05, 0.1, 0.5 mg/ml) in comparison with control (PBS/ phosphate buffer saline) both in vivo and in vitro. In vivo study involved the cytogenetic evaluation of cabergoline in mice by examination of mitotic index percentage (MI), micronucleus formation (MN) and chromosomal aberrations. Result indicated that all the tested doses cause significant reduction in MI percentage, while significant rise was seen with both MN formation and all studied chromosomal aberrations. While in vitro study involved measuring the effect of cabergoline on normal cell line (REF/ Rat embryonic

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Publication Date
Wed Jun 01 2022
Journal Name
Journal Of The College Of Languages (jcl)
A Feminist Stylistic Analysis of Anti-feminist Poetry in English and Arabic

Language plays a major role in all aspects of life. Communication is regarded as the most important of these aspects, as language is used on a daily basis by humanity either in written or spoken forms. Language is also regarded as the main factor of exchanging peoples’ cultures and traditions and in handing down these attributes from generation to generation. Thus, language is a fundamental element in identifying peoples’ ideologies and traditions in the past and the present. Despite these facts, the feminist linguists have objections to some of the language structures, demonstrating that language is gender biased to men. That is, language promotes patriarchal values. This pushed towards developing extensive studies to substantiate s

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Crossref
Publication Date
Wed Dec 15 2021
Journal Name
Al-adab Journal
A Feminist Rhetorical Analysis of Anti-feminist Poetry in English and Arabic

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Publication Date
Mon May 06 2024
Journal Name
Journal Of Pakistan Association Of Dermatologists
Assessment of tumor necrosis factor alpha and interleukinـ10 in obese psoriatic patients before and after using apremilast

Background Psoriasis is one of the most prevalent chronic inflammatory skin conditions; its prevalence ranges from 1 to 3%. Tumor necrosis factor-alpha (TNF-α), a cytokine that enhances inflammation, is overexpressed in synovium and skin plaques in psoriasis. TNF-α plays a critical role in the pathogenesis of psoriasis. IL-10 is the most crucial cytokine for reducing excessive immune responses and decreasing pro-inflammatory reactions in all autoimmune disorders.   Objective To evaluate the effect of Apremilast on ILـ10, TNFـα, and BMI in obese psoriatic patients.   Methods Thirty patients included in this investigative study to measure the concentrations of TNFـα, ILـ10 and BMI, before and after receiving Apremilast. TNFـα and

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