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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
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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
Thu Aug 01 2024
Journal Name
Journal Of Ecological Engineering
Synthesis and Characterization of Acidic Activated Carbon from Corncobs for Adsorption Desulfurization of Simulated Crude Oil
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Corncob is an agricultural biomass waste that was widely investigated as an adsorbent of contaminants after transforming it into activated carbon. In this research carbonization and chemical activation processes were achieved to synthesize corncob-activated carbon (CAC). Many pretreatment steps including crushing, grinding, and drying to obtain corncob powder were performed before the carbonization step. The carbonization of corncob powder has occurred in the absence of air at a temperature of 500 °C. The chemical activation was accomplished by using HCl as an acidic activation agent. Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), X-ray diffraction (XRD), and Brunauer–Emmett–Teller (BET) facilitate

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
Evaluation of Laser Doping of Si from MCLT Measurement
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The measurement of minority carrier lifetime (MCLT) ofp-n Si fabricated with aid of laser doping technique was reported. The measurement is achieved by using open circuit voltage decay (OCVD) technique. The experiment data confirms that the value of MCLT and proftle of Voc decay were very sensitive to the doping laser energy.

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Publication Date
Sun Jan 26 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Evaluation of Financial Performance of the Iraqi Insurance Company
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Insurance Companies perform a prominent role in providing services and bolstering national economy, and they contribute in achieving the aims of the economic development plans in addition to many other social and economic benefits. So it is necessary to evaluate the activity of these companies continuously to define performance level and its nature. Financial analysis is one of the important instruments that helps in analyzing and explanation of data in such a way that enable administration to define performance level and diagnosing strength and weakness points. This study tackles the state of affairs of the Iraqi Insurance Company which is considered as one of the active national institutions, due to its distinguished role in collecting

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Publication Date
Wed Jun 20 2012
Journal Name
Journal Of Biotechnology Research Center
Evaluation of toxic effects of two weight reduction pills
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Abstract his study involved evaluation of side effects of two weight reduction pills that had been widely distributed in the last period. Two weight reduction compounds are studied, Reductil (containing chemical substances) and Chinese’s weight reduction herbs (containing natural substances). Two doses for each compound are used in this research; 5mg/ml and 0.5mg/ml for Reductil, while 30mg/ml and 10mg/ml for Chinese weight reduction herbs. To evaluate the toxic effects of these compounds, the following parameters were determined which include mitotic index (cytogenetic analysis), serum FSH and LH hormones level (follicles stimulation hormone/FSH and lutenising hormone/LH) and histological examination of female mice ovaries. Control group

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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
Thu Feb 01 2024
Journal Name
Baghdad Science Journal
Mangrove Landscaping As An Adaptation Pattern To Reduce The Impact of Climate Change in Segara Anakan Lagoon, Cilacap Regency Indonesia
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Mangrove landscaping in the Segara Anakan Lagoon (SAL) is an adaptation pattern of mangrove ecosystems to live and grow in unstable areas. This research aimed to develop a mangrove landscape to mitigate the impacts of ocean waves, currents, and inundation due to climate change. The study was conducted in SAL and Cilacap Coast (CC) using the environmental properties and climate change data. The data obtained were analyzed using mapping and trendline analyses. The results showed that mangrove landscaping in Segara Anakan had four zones with Nypa frutican, Rhizophora styllosa, Aegiceras corniculatum, Rhizophora apiculata, Avicennia marina, Sonneratia alba identified as the best adaptation of mangrove species. Climate change give a high impa

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Publication Date
Fri Jan 01 2016
Journal Name
Iraqi Journal Of Science
Effect of growth media components and growth condition on indole - 3 - acetic acid (IAA) production by Pseudomonas putida isolated from soil
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Publication Date
Fri Sep 01 2023
Journal Name
Al-khwarizmi Engineering Journal
Green Fabrication and Characterization of Zinc Oxide Nanoparticles using Eucalyptus Leaves for Removing Acid Black 210 Dye from an Aqueous Medium
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This study uses an environmentally friendly and low-cost synthesis method to manufacture zinc oxide nanoparticles (ZnO NPs) by using zinc sulfate. Eucalyptus leaf extract is an effective chelating and capping agent for synthesizing ZnO NPs. The structure, morphology, thermal behavior, chemical composition, and optical properties of ZnO nanoparticles were studied utilizing FT-IR, FE-SEM, EDAX, AFM, and Zeta potential analysis. The FE-SEM pictures confirmed that the ZnO NPs with a size range of (22-37) nm were crystalline and spherical. Two methods were used to prepare ZnO NPs. The first method involved calcining the resulting ZnO NPs, while the second method did not. The prepared ZnO NPs were used as adsorbents for removing acid black 210

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Publication Date
Mon Feb 18 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Evaluation of Proceedings External Oversight on Investment Budget Projects for local Governments: "Applied Research in The Government of The Province of Dhi Qar local"
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The investment budget represents a stage of the investment decision in service units, and the preparation and implementation needs to be a complement of the same planning part, because the planning does not end with the development of the plan, but includes a follow-up implementation, so it has to be effective and efficient oversight of the estimates and procedures for disbursement of funds approved for investment projects, The problem with research in that local governments suffer from the presence of Allkaat and problems facing the implementation of the investment budget projects due to the adoption budget items which can not be measured the efficiency of the performance of these units of government by, and shortcomings in the control

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Publication Date
Mon Nov 01 2021
Journal Name
Journal Of Ecological Engineering
Calibration and evaluation of aquacrop for maize (Zea Mays L.) under different irrigation and cultivation methods
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rop simulation models play a pivotal role in evaluating irrigation management strategies to improve water use in agriculture. The aim of this study is to verify the validity of the Aquacrop model of maize under the surface and sprinkler irrigation systems, and a cultivation system, borders and furrows, and for two varieties of Maze (Fajr and Drakma) At two different sites in Iraq, Babylon and Al-Qadisiyah governorates. An experiment was conducted to evaluate the performance of the Aquacrop model in simulating canopy cover (CC), biomass (B), dry yield, harvest index (HI), and water productivity (WP). The results of RMSE, R2, MAE, d, NSE, CC, Pe indicated good results and high compatibility between measured and simulated values. The highest a

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