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.
A tetradentate (N2O2) Schiff base (H2Ldfm) was successfully synthesized via condensation of curcumin / diferuloylmethane (dfm) and L-leucine amino acid (HL). There were three different methods that used for synthesizing H2Ldfm; (refluxing, grading, and fusion). Ten different metal complexes were also successfully synthesized by combination of the Schiff base (H2Ldfm) and 1,10-phenanthroline (phen) ligand to form a hexadentate (N4O2) mixed ligands (Ldfm , phen) with ten different metal salts (M) where{ M= Al(III), Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Ag(I), Cd(II), Hg(II), and Pb(II)}. The molar ratio of reactants was (1:1:1) (M: H2Ldfm : phen). The new Schiff base and its new complexes were characterized by different physicochemical tec
... Show Moreوفقأ للدراسات السابقة تم تحضير ليكاند آزو جديد (ن-(3-اسيتايل-2-هيدروكسي-5-مثيل-فنيل)ن-(4-كاربوكسي-سايكلوهكسيل مثيل)-ملح الدايازونيوم) وبعد التحقق من الصيغة المقترحة وفق نتائج التحاليل وبعد استخدام الليكاند لتحضير سلسلة ن المعقدات باستخدام نسب مولية متساوية (1:1) من الليكاند وتفاعلها مع كل من املاح المنغنيز والكوبلت والنيكل والنحاس والخارصين وبعد التحقق وفق تقنيات التحاليل الطيفية والتشخيصية(الاشعة فوق البنف
... Show MoreThe present work involved synthesis of serval new substituted tetrazole via Schiff bases for trimethoprim drug by two steps. The first step involved direct reaction of different ketones and aldehydes with trimethoprim producing the corresponding Schiff bases (1-10), whereas the second step, involved preparation new tetrazoles derivatives (11-20) through reaction of the ready Schiff bases (in the first step) with sodium azidein in dioxin. The prepared compounds were characterized by UV, FT-IR, and some of them by 13C-NMR, 1H-NMR spectroscopy and physical properties.
A new 5‐fluorouracil–naproxen conjugate is synthesized as a mutual prodrug for targeting cancer tissues. The structure of the target compound and their intermediate are characterized by their melting point, IR, 1H NMR, 13C NMR, and elemental microanalysis. The cytotoxic activity is preliminarily evaluated using nonsmall lung cancer CRL‐2049, human breast cancer CAL‐51, and one type of normal cell line; rat embryo fibroblast cell line. The synthesized compound shows a good cytotoxic effect at the cancer cell and no significant effect at rat embryo fibroblast cell line.
The 3D electro-Fenton technique is, due to its high efficiency, one of the technologies suggested to eliminate organic pollutants in wastewater. The type of particle electrode used in the 3D electro-Fenton process is one of the most crucial variables because of its effect on the formation of reactive species and the source of iron ions. The electrolytic cell in the current study consisted of graphite as an anode, carbon fiber (CF) modified with graphene as a cathode, and iron foam particles as a third electrode. A response surface methodology (RSM) approach was used to optimize the 3D electro-Fenton process. The RSM results revealed that the quadratic model has a high R2 of 99.05 %. At 4 g L-1 iron foam particles, time of 5 h, and
... Show MoreThe prostaglandins inside inflamed tissues are produced by cyclooxygenase-2 (COX-2), making it an important target for improving anti-inflammatory medications over a long period. Adverse effects have been related to the traditional usage of non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of inflammation, mainly centered around gastrointestinal (GI) complications. The current research involves the creation of a virtual library of innovative molecules showing similar drug properties via a structure-based drug design. A library that includes five novel derivatives of Diclofenac was designed. Subsequently, molecular docking through the Glide module and determining the binding free energy implementing the P
... Show MoreThis study was aimed to assess the impact of vermicompost, glutathione, and their interaction on beetroot (Beta vulgaris L.) growth, yield, and antioxidant traits. The experiment carried out at vegetable field of the College of Agricultural Engineering Sciences - University of Baghdad during fall season 2019. The experiment was conducted using factorial arrangement within Randomized Complete Block Design with two factors and three replicates (3X3X3). Applying vermicompost before cultivation represented the first factor (0, 15, 30 ton.ha-1), which symbolized (V0, V1, V2). Glutathione (0, 75, 150 mg.L-1) which symbolized (G0, G1, G2) represented the second factor. Results showed the superiority of secondary interaction treatment V2G2
... Show MoreThe present work aims to study the efficiency of using aluminum refuse, which is available locally (after dissolving it in sodium hydroxide), with different coagulants like alum [Al2 (SO4)3.18H2O], Ferric chloride FeCl3 and polyaluminum chloride (PACl) to improve the quality of water. The results showed that using this coagulant in the flocculation process gave high results in the removal of turbidity as well as improving the quality of water by precipitating a great deal of ions causing hardness. From the experimental results of the Jar test, the optimum alum dosages are (25, 50 and 70 ppm), ferric chloride dosages are (15, 40 and 60 ppm) and polyaluminum chloride dosages were (10, 35 and 55 ppm) for initial water turbidity (100, 500 an
... Show MoreMetal oxide nanoparticles, including iron oxide, are highly considered as one of the most important species of nanomaterials in a varied range of applications due to their optical, magnetic, and electrical properties. Iron oxides are common compounds, extensive in nature, and easily synthesized in the laboratory. In this paper, iron oxide nanoparticles were prepared by co-precipitation of (Fe+2) and (Fe+3) ions, using iron (II and III) sulfate as precursor material and NH4OH solution as solvent at 90°C. After the synthesis of iron oxide particles, it was characterized using X-ray diffraction (XRD), infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). These tests confirmed the obtaining o
... Show More