Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenocarcinoma and mouse hepatoblastoma cells with low cytotoxic effect against normal human breast cells. Their binding mode to the active site of several histone deacetylases has been studied by docking and the results gave a preliminary indication that they could be successful histone deacetylase inhibitors.
In light of increasing demand for energy consumption due to life complexity and its requirements, which reflected on architecture in type and size, Environmental challenges have emerged in the need to reduce emissions and power consumption within the construction sector. Which urged designers to improve the environmental performance of buildings by adopting new design approaches, Invest digital technology to facilitate design decision-making, in short time, effort and cost. Which doesn’t stop at the limits of acceptable efficiency, but extends to the level of (the highest performance), which doesn’t provide by traditional approaches that adopted by researchers and local institutions in their studies and architectural practices, limit
... Show MoreThe concept of the order sum graph associated with a finite group based on the order of the group and order of group elements is introduced. Some of the properties and characteristics such as size, chromatic number, domination number, diameter, circumference, independence number, clique number, vertex connectivity, spectra, and Laplacian spectra of the order sum graph are determined. Characterizations of the order sum graph to be complete, perfect, etc. are also obtained.
A series of benzohydrazide derivatives attached to coumarin moiety at position 6 and 7 have been synthesized. The reaction of coumarin derivatives (coumarin I and II) with p-nitrophenyl hydrazine yield Schiff bases (compound1a and IIa).These Schiff bases were refluxed with benzoyl chloride to give benzohydrazide derivatives of coumarin substituted at its 6 or 7 nucleus position (Ia1 and IIa1).The reaction and the purity of the products were checked by thin layer chromatography (TLC). The structures of the final compounds and their intermediates were confirmed by their melting points, infra red spectroscopy, and elemental microanalysis(CHN).
Compounds (Ia1 and IIa1) were evaluated for&n
... Show MoreIn this work, novel compounds of hydrazones derived from (2,4-dinitrophenyl) hydrazine were synthesized. Benzamides derivatives and sulfonamides derivatives were prepared from p-amino benzaldehyde. Then these compounds were condensed with (2,4-dinitrophenyl) hydrazine through Imine bond formation to give hydrazones compounds. The compounds were characterized using FT-IR (IR Affinity-1) spectrometer, and 1HNMR analyses. The majority of the compounds have a moderate antimicrobial activity against “Gram-positive bacteria staphylococcus Aureus, and staphylococcus epidermidis, Gram-negative bacteria Escherichia coli, and Klebsiella pneumoniae, and fungi species Candida albicans” using concentrations of 250 µg\ml.
Five novel nickel, iron, cobalt, copper, and mercury complexes were synthesized from tetraazamacrocyclic Schiff base ligand (L), which were derived from 3-(4-(dimethyl amino) benzylidene) pentane-2,4-dione and 1,2- diaminocyclohexane in a 2:2 molar ratio. Many physico-chemical and spectroscopic techniques, including melting point, 1HNMR, 13CNMR, elemental analysis, molar conductance, magnetic susceptibility, UV-Vis, FT-IR, and thermogravimetric analysis (TGA), were used to characterize the Schiff base ligand and all metal complexes. The octahedral geometry of all the complexes [MLCl2] is confirmed by spectroscopic analyses. All substances' biological properties, such as their in vitro antioxidant activity or level of free radical scavenging
... Show MoreThis study includes design and synthesis of new non-steroidal anti-inflammatory agents (NSAIDs) with expected cyclooxygenase-2 (COX-2) selective inhibition to achieve better activity and low gastric side effects. Two series of compounds have been designed and synthesized as potential NSAIDs,these are: Salicylamide derivatives (compounds 3,4,5 ) and Diflunisal derivatives (compounds 10&11). In vivo acute anti-inflammatory effect of one of the synthesized agents (compound 3) was evaluated in the rat using egg-white induced paw edema model of inflammation. Preliminary pharmacological study revealed that compound 3 exhibited less anti-inflammatory effect compared to that of aspirin after
... Show MoreHybrid architecture of ZnO nanorods/graphene oxide ZnO-NRs@GO synthesized by electrostatic self-assembly methods. The morphological, optical and luminescence characteristics of ZnO-NRs@GO and ZnO-NRs thin films have been described by FESEM, TEM, HRTEM, and AFM, which refers to graphene oxide have been coated ZnO-NRs with five layers. Here we synthesis ZnO-NRs@GO by simple, cheap and environmentally friendly method, which made it favorable for huge -scale preparation in many applications such as photocatalyst. ZnO-NRs@GO was applied as a photocatalyst Rodamin 6 G (R6G) dye from water using 532 nm diode laser-induced photocatalytic process. Overall degradation of R6G/ ZnO-NRs@GO was achieved after 90 minutes of laser irradiation while it ne
... Show MoreThe Character is one of the elements of Storytelling, as it is the center of the plot, making it the basis on which the talk is about. The talk is the portrayal of the character while they’re acting; the novelist presents the character by interacting with the events, and the extent of the negative and positive appearing impact on the character. It should be noted that everyone has two personalities or more, each one appearing in a different position or situation. For instance, a man can be a father, a lover, an employee, a son or anyone else .. in another position, he might be a master, and in another a looser begging for the mercy of his humiliator, and sometimes he can show weakness to the one he loves, or show strength to his enemie
... Show MoreBackground: Human semen contains high concentrations of fructose, zinc (Zn) and copper (Cu) in bound and ionic forms for Zn and Cu. The presence of abnormal levels of fructose and those trace elements may affect spermatogenesis with regard to production, maturation, motility and fertilizing capacity of the spermatozoa.Objective: To evaluate the levels of fructose, Zn and Cu in seminal plasma in different groups of male infertility and to correlate their concentrations with various sperm parameters.Methods: The concentrations of fructose, Zn and Cu were measured in 114 semen samples from normozoospermic, oligozoospermic, astheno-zoospermic, and azoospermic men using the electrothermal-atomic absorption spectrometry for Zn and Cu determinatio
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