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.
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... Show MoreA new 4-thiazolidinone, substitutedbenzylidene-thiazolidinone and tetrazole were synthesized from thiosemicarbazone and hydrazone. The thiosemicarbazone was prepared by the reaction of thiosemicarbazide with aldehyde derivative from L-ascorbic acid in absolute ethanol using glacial acetic acid as a catalyst. 1, 3-thiazolidin-4-ones were synthesized from the condensation of thiosemicarbazones with chloroacetic acid in presence of anhydrous sodium acetate. A 1, 3- thiazolidine-4-one was reaction with several 4-substitutedaldehydes to produce new derivatives with a double bond at the position-5 of the 4-thiazolidinone ring. While the tetrazole compounds were synthesized by 1, 3-cycloaddition reaction of sodium azide and hydrazone compounds in
... Show MoreBackground: Bone regeneration in dehiscence and fenestration defect can be improved with the use of platelet rich fibrin (PRF) that provides a scaffold for new bone regeneration. This study was conducted to assess the effectiveness of PRF as a graft material and membrane in dehiscence and fenestration defects. Materials and Methods: This prospective clinical study included patients who received dental implants that demonstrated peri-implant defects which were augmented using Leukocyte- PRF (L-PRF) or Advanced-PRF (A-PRF). Twenty four weeks postoperatively the defect resolution and the density of regenerated bone were assessed by CBCT and re-entry surgery. The assessment also included measurement of primary and secondary implant stability
... Show MoreKey words:Jasminumsambac, Volatile oil, Antioxidant.
High performance liquid chromatography was applied for the separation and identification of four antharquinone derivatives, aloe emodin, emodin, chrysophanol and physcion. The separation was carried out using Eurospher 100, C18 column (4.6 mm i.d. x 250 mm, 5 µm) under the following conditions: acetonitile (solvent A) and water: acetic acid (99.9: 0.1 v/v, pH 3.5)( solvent B) as a mobile phase with isocratic elution with 30% solvent B at flow rate 0.8 ml/min. The detection wavelength was set at 254 nm. The four antharquinone derivatives were isolated from the Iraqi rhubarb, Rheum ribes root by preparative TLC, their structures were identified by 1H NMR and used as standards for HPLC analysis. The percentages of alo
... Show MoreThe article presents the synthesis and liquid crystalline properties of some of new bent and linear core compounds containing a 1,3,4-oxadiazole, piperazine and thiazolidin-4-one rings as a central core. The new synthesized compounds were characterized by elemental analysis and FTIR, ¹HNMR and mass spectroscopy). The liquid crystalline properties were studied by polarized optical microscopy and differential scanning calorimetry. All Schiff bases compounds with 1,3,4-oxadiazole and piprzaine ring in central core presented liquid crystalline properties. The liquid crystallinity of compounds containing 1,3,4-oxadiazole and thiazolidin-4-one rings as a central core were found depending on the type of terminal substituents.