Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds were synthesized and characterized by successfully by ART-FTIR, NMR and ESI- Ms. Assessed for their cytotoxic activity against human colon adenocarcinoma MCF-7 (IC50, I=105.15, II=60.00, III=54.11, IV=56.57, vorinostat=28.41) and hepatoblastoma HepG2 (IC50, I=63.91, II=135.18, III=118.85, IV=51.46, vorinostat=37.50). Most of them exhibited potent HDAC inhibitory activity and significant cytotoxicity. Conclusions: The synthesized compounds (I, II, III and IV) showed cytotoxicity toward MCF-7 and HepG2 cancer cell lines and their docking analysis provided a preliminary indication that they are viable [HDAC6] candidates.
Ondansetron hydrochloride (ONH) is a very bitter, potent antiemetic drug used for the treatment and/or prophylaxis of chemotherapy or radiotherapy or postoperative induced emesis. The objective of this study is to formulate and evaluate of taste masked fast dissolving tablet (FDTs) of ONH to increase patient compliance.
ONH taste masked granules were prepared by solid dispersion technique using Eudragit E100 polymer as an inert carrier. Solvent evaporation and fusion melting methods were used for such preparation.
Completely taste masking with zero release of drug in phosphate buffer pH 6.8was obtained from granules prepared by solvent evaporation method using drug: polymer ratio of 1:2, from which four formulas pas
... Show MoreA new ligand N-(methylcarbamothioyl) acetamide (AMP) was synthesized by reaction of acetyl chloride with adenine. The ligand was characterized by FT-IR, NMR spectra and the elemental analysis. The transition metal complexes of this ligand where synthesize and characterized by UV-Visible spectra, FT-IR, magnetic suscepility, conductively measurement. The general formula [M(AMP)2Cl2], where M+2 = (Mn, Co, Ni, Cu, Zn, Cd, Hg).
Liquid-crystalline organic semiconductors exhibit unique properties that make them highly interesting for organic optoelectronic applications. Their optical and electrical anisotropies and the possibility to control the alignment of the liquid-crystalline semiconductor allow not only to optimize charge carrier transport, but to tune the optical property of organic thin-film devices as well. In this study, the molecular orientation in a liquid-crystalline semiconductor film is tuned by a novel blading process as well as by different annealing protocols. The altered alignment is verified by cross-polarized optical microscopy and spectroscopic ellipsometry. It is shown that a change in alignment of the
The technological development in the field of information and communication has been accompanied by the emergence of security challenges related to the transmission of information. Encryption is a good solution. An encryption process is one of the traditional methods to protect the plain text, by converting it into inarticulate form. Encryption implemented can be occurred by using some substitute techniques, shifting techniques, or mathematical operations. This paper proposed a method with two branches to encrypt text. The first branch is a new mathematical model to create and exchange keys, the proposed key exchange method is the development of Diffie-Hellman. It is a new mathematical operations model to exchange keys based on prime num
... Show MoreFour antimony compounds were used in this inves as additives to retard combustion of unsaturated polyester and epoxy resins, namely: 1. Tetraethyl ammonium tribromoethylantimonates (additive I). 2. Tetraethyl ammonium chlorodibromoethylantimonates (additive II). 3. Tetraethyl ammonium trichloroethylantimonates (additive III). 4. Tetraethyl ammonium bromodichloroethylantimonates (additive IV). The effects of these additives on flammability of unsaturated polyester and epoxy resins have been studied by using sheets of the resins with weight percentages of (0.5,1.0,1.5,2.0,2.5&3.0%) of the additives in dimensions of (150 X150X3)mm .Three standard test methods were used to measure the flame retardation which are: (ASTM:D -2863), (ASTM:D-635
... Show MoreIn this work, the effects of solvent properties on the characteristics of absorption and fluorescence for two laser dyes was studied. Dyes used in this work include Coumarin 5400 and DCM, while the solvents include ethanol, methanol, acetone, propanol and chloroform. Coumarin 5400 dye shows sharp fluorescence peaks in the green band of visible region while the DCM dye shows relatively wide band within 590-630 nm. Therefore, the selection of any dye for random gain medium applications should be performed after determining the most appropriate solvent as the optimum fluorescence characteristics are obtained.
Background: obesity is a major global health problem with more than 200 million obese men and almost 300 million obese women. Melatonin is a well-known molecule for its involvement in circadian rhythm regulation and has multiple pathological actions including control of appetite, sleep wake cycle and metabolic syndrome.
Aim: to estimate the effect of melatonin supplements on obese patients on a calorie restricted diet in comparison to patients on lifestyle measures only in the form of weight loss, waist circumference and sleep quality.
Subjects and Method: one hundred patients with body mass index > 24 were collected, fifty patients were starte
... Show MoreThe theory of the psychologist’s Piaget states that man passes through four stages; other says that mankind passes through five. At each stage, human learn new characteristics, values, skills, and cultures from different environment that differ from one society to another. Therefore, the cultures of societies vary according to the diversity of the environments. These environments also vary depending on the circumstances surrounding them, e.g., in war environment, the individual learns what he does not learn from living in safe environment. As the environment changes, the communicative message also changes. This message is subject to person, groups, organizations and parties and directed to a diverse audience in its orientations and bel
... Show MoreThis study aims to answer a significant problem of social sciences and philosophy: How do we construct an institutional reality such as diplomacy with an objective recognizable existence? The study assumes that the ability to build institutional reality is based on our biological capacity, as it takes different forms in all the institutions we construct. The study takes the theory of the American philosopher John Searle as an approach to examining the assumption. The study sums up important findings; cultures, although they share the biological capacity on which they produce institutional realities, differ in the form of the value standards on which the institutional realities are based. The study recommends the need of Arab social resea
... Show MoreAmino glycoside derivation including, Neomycin, Streptomycin, Kanamycin and Gentamycin with special reagents, which are benzoylchloride; benzene sulfonyl chloride and phthalic anhydride were made to enhance Uv-detectability for HPLC analysis. But there are many problems facing pre column derivation and in order to solve this, the conductivity of antibiotic derivatives were used to calculate the dissociation constant and the hydrolysis rate which determined concern type reaction. In addition the characteristics those controlling the hydrolysis of antibiotic-derivatives were investigated.