Coumarins have been recognized as anticancer competitors. HDACis are one of the interesting issues in the field of antitumor research. In order to achieve an increased anticancer efficacy, a series of hybrid compounds bearing coumarin scaffolds have been designed and synthesized as novel HDACis, In this review we present a series of novel HDAC inhibitors comprising coumarin as a core e of cap group of HDAC inhibitors that have been designed, synthesized and assessed for their enzyme inhibitory activity as well as antiproliferative activity. Most of them exhibited potent HDAC inhibitory activity and significant cytotoxicity
This research involves the synthesis of some sulphanyl benzimidazole derivatives (Ia-c), which were prepared from reaction of 2-mercaptobenzimidazole substituted benzyl halide, and structures were identified by spectral methods[FTIR, 1H-NMR and 13C-NMR].These compounds were investigated as corrosion inhibitors for carbon steel in 1M H2SO4 solution using weight loss, potentiostatic polarization methods; obtained results showed that the sulphanyl benzimidazole derivatives retard both cathodic and anodic reactions in acidic media, by virtue of adsorption on the carbon steel surface. This adsorption obeyed Langmuir’s adsorption isotherm. The inhibition efficiency of (Ia-c) ranging between (65-92) %. By using different Ib derivative concent
... Show MoreIn this work, we synthesized thirteen compounds of 1-(2-furoyl)thiourea derivatives 1-13 by conversion of 2-furoyl chloride to 2-furoyl isothiocyanate by reacting it with potassium thiocyanate in dry acetone in a quite short reflux time then, in the same pot, different of (primary and secondary amines) were added individually to achieve thiourea derivatives. The products were characterized spectroscopically using (FT-IR, 1H NMR and 13C NMR) techniques. Some of them were evaluated as antioxidant agents using DPPH radical scavenging method, and all were examined theoretically as enzyme inhibitors against Bacillus pasteurii urease (pdb id: 4ubp) and by studying molecular docking using Autodock (4.2.6) software.
Sildenafil, tadalafil, and vardenafil are phosphodiesterase type 5 enzyme (PDE-5) inhibitors used for the treatment of male erectile dysfunction. This present study aims to investigate 55 herbal products indicated for men’s sexual health from the Malaysian market for adulteration of PDE-5 inhibitors and analogues. The screening and identification of 20 PDE-5 inhibitors and analogues in herbal products of various forms (powder, capsules, tablets, and pastels) were conducted using gas chromatography–electron impact-mass spectrometer (GC-EI-MS). The analysis has shown that 19 herbal products were adulterated with PDE-5 inhibitors and analogues. Unique ion fragmentations and the presence of molecular
... Show MoreAllosteric 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.
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
Mobile-based human emotion recognition is very challenging subject, most of the approaches suggested and built in this field utilized various contexts that can be derived from the external sensors and the smartphone, but these approaches suffer from different obstacles and challenges. The proposed system integrated human speech signal and heart rate, in one system, to leverage the accuracy of the human emotion recognition. The proposed system is designed to recognize four human emotions; angry, happy, sad and normal. In this system, the smartphone is used to record user speech and send it to a server. The smartwatch, fixed on user wrist, is used to measure user heart rate while the user is speaking and send it, via Bluetooth,
... Show MoreMetaheuristic is one of the most well-known fields of research used to find optimum solutions for non-deterministic polynomial hard (NP-hard) problems, for which it is difficult to find an optimal solution in a polynomial time. This paper introduces the metaheuristic-based algorithms and their classifications and non-deterministic polynomial hard problems. It also compares the performance of two metaheuristic-based algorithms (Elephant Herding Optimization algorithm and Tabu Search) to solve the Traveling Salesman Problem (TSP), which is one of the most known non-deterministic polynomial hard problems and widely used in the performance evaluations for different metaheuristics-based optimization algorithms. The experimental results of Ele
... Show MoreThe rapid development of automation industries and technologies has shown incredible prospects for transforming our homes into a smart home automation system, which are more secure than a simple home. This paper proposes a home application based on voice and text called the Automated Control and Monitoring System (ASCM). This application can be utilized by both normal and vision-impaired people by using with a mobile phone.
The application allows users to send voice commands through Google Assistant installed on Android to control the appliances. They can also have complete monitoring by logging onto the ThingSpeak dashboard, which displays a device status indicator and sends alert messages in the event of dang
... Show MoreSeveral recent approaches focused on the developing of traditional systems to measure the costs to meet the new environmental requirements, including Attributes Based Costing (ABCII). It is method of accounting is based on measuring the costs according to the Attributes that the product is designed on this basis and according to achievement levels of all the Attribute of the product attributes. This research provides the knowledge foundations of this approach and its role in the market-oriented compared to the Activity based costing as shown in steps to be followed to apply for this Approach. The research problem in the attempt to reach the most accurate Approach in the measurement of the cost of products from th
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