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.
Obesity is an escalating health problem in developing countries. One to ten children worldwide are overweight in a report showed by the International Obesity Task Force. Ghrelin, orexigenic peptide, has 28 amino acids, it is considered the greatest remarkable promotion in the last two decades for understanding the physiological changes of action regulating food intake and hunger. Obestatin is a 23-amino acid peptide nearly connected to ghrelin that secures from substitutio
... Show MoreThe possibility of using activated carbon developed from date palm seeds wastes as a permeable reactive barrier (PRB) to remove copper from polluted shallow groundwater was investigated. The activated carbon has been developed from date palm seeds by dehydrating methods using concentrated sulfuric acid. Batch tests were performed to characterize the equilibrium sorption properties of new activated carbon in copper-containing aqueous solutions, while the sandy soil (aquifer) was assumed to be inert. Under the studied conditions, the Langmuir isotherm model gives a better fit for the sorption data of copper by activated carbon than other models. At a pilot scale, One-dimensional column experiments were performed, and an integrated model ba
... Show MoreThe δ-mixing of γ-transitions in 70As populated in the 32 70 70 33 Ge p n As (, ) γ reaction is calculated in the present work by using the a2-ratio methods. In one work we applied this method for two cases, the first one is for pure transition and the sacend one is for non pure transition, We take into account the experimental a2-coefficient for previous works and δ -values for one transition only.The results obtained are, in general, in a good agreement within associated errors, with those reported previously , the discrepancies that occur are due to inaccuracies existing in the experimental data of the previous works.
Silymarin (SM) is a plant extract obtained from Silybum marianum( milk thistle) . It is class II type drug according to Biopharmaceutics Classification System with low bioavailability due to its low solubility.
Micro/nanonization during crystallization, surface modification and crystal structure modification may improve the dissolution rate of poorly water-soluble drugs.
The aim of this study was to increase the water solubility and dissolution rate of SM by in-situ micronization using solvent change either by stirring or ultrasonic method. Stabilizers like Gelatin, PVP-K30, HPMC15, Pulullan were used to stabilize the prepared ultrafine crystals. Effect of type and concentration of hydrophilic polymer, solv
... Show MoreBackground: Sliding mechanics is widely used during orthodontic treatment. One of the disadvantages of this mechanics is the friction generated at the bracket/archwire interface, which may reduce the amount of desired orthodontic movement obtained. The aim of the present in vitro study was to evaluate and compare the static frictional forces produced by two passive self-ligating brackets stainless-steel and hybrid and two conventional brackets stainless-steel and monocrystal ligated with stainless-steel ligature wire at two degrees of torque(zero and twenty) under dry condition. Materials and method: One hundred and sixty brackets were used in this study divided into four groups each group consisted of forty brackets these are: Two self-li
... Show More“Orodispersible Tablet†a tablet that is to be placed in oral cavity where it disperses rapidly by saliva with no need for water before swallowing. Zaltoprofen (ZLP) is one of NSAIDs which is used in the treatment of rheumatoid arthritis and osteoarthritis as well as to relieve inflammation and pain after surgery, injury and tooth extraction. The present study was aimed to prepare rapidly dissolved lyophilized Zaltoprofen tablet with different pharmaceutical excipients and studying the factors affecting pharmaceutical properties like (solubility, disintegration time DT, dissolution, etc.) of tablets. The lyophilized disintegrating tablets (LDTs) were prepared using Zydis technique by lyophilization an aqueous
... Show MoreThe study's primary purpose is to explore an appropriate way of monitoring and assessing water depths using the satellite remote sensing technique of the Al Habbaniyah Lake in Iraq. This research studied the experience-conditions (thresholds) of different bands for multi-temporal satellite image data with different satellite image sensors (Landsat 5-TM, and EO1-ALI) for the same region, to recognize regions of water depths. The threshold values are taken that to separate the Al Habbaniyah Lake to the required depths (shallow, deep, and very deep), as a supervised method. A three-dimension feature space plot had used to represent these regions. The relationship of the mean values of the three separated water regions with all TM and A
... Show MoreThe present work included study of the effects of weather conditions such as solar radiation and ambient temperature on solar panels (monocrystalline 30 Watts) via proposed mathematical model, MATLAB_Simulation was used by scripts file to create a special code to solve the mathematical model , The latter is single –diode model (Five parameter) ,Where the effect of ambient temperature and solar radiation on the output of the solar panel was studied, the Newton Raphson method was used to find the output current of the solar panel and plot P-V ,I-V curves, the performance of the PV was determined at Standard Test Condition (STC) (1000W/m2)and a comparison between theoretical and experimental results were done .The best efficiency
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