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.
The increase in population resulted in an increase in the consumption of water. The present work investigates the performance of a recycling solar- powered greywater treatment system for the purposes of irrigation, used to reduce the amount of waste grey water and reduce electricity consumption and reduce the costs of constructing large scale water treatment plants. The system consumes about 3814W per hour and provides water treatment about 1.4 m3 per day. The proposed system is designed to residential, office and governmental buildings application. Tests are conducted in an office building at the Ministry of Science and Technology site in Baghdad. Laboratorial water samples testing analyses are co
... Show MoreCiprofloxacin is widely used in treating adults infected with Gram-negative bacteria. It is contraindicated in children, growing adolescents and during pregnancy due to joint toxicity. Its toxicity concerning other organs needs to be clarified. Thus, this study was designed to study the possible cardiac damage induced by two selected doses of ciprofloxacin in juvenile rats.Eighteenth healthy juvenile rats (4 weeks old and their weight 30 ± 2 gm) were utilized in this study and divided into three groups. Group-I control; group II and group III, respectively injected IP with 25 mg/kg and 50 mg/kg ciprofloxacin every 12 hours for one week. Serum enzymes activities alanine aminotransferase (ALT), aspartate aminotransferase (AST), cr
... Show MoreObjective: The objective of the present study was to design and optimize oral fast dissolving film (OFDF) of practically insoluble drug lafutidine in order to enhance bioavailability and patient compliance especially for a geriatric and unconscious patient who are suffering from difficulty in swallowing.Methods: The films were prepared by a solvent casting method using low-grade hydroxyl propyl methyl cellulose (HPMC E5), polyvinyl alcohol (PVA), and sodium carboxymethyl cellulose (SCMC) as film forming polymers. Polyethylene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer to enhance the film forming properties of the polymer. Tween 80 (1% solution) and poloxamer407 were used as a surfactant, citri
... Show MoreABSTRACT
Naproxen(NPX) imprinted liquid electrodes of polymers are built using polymerization precipitation. The molecularly imprinted (MIP) and non imprinted (NIP) polymers were synthesized using NPX as a template. In the polymerization precipitation involved, styrene(STY) was used as monomer, N,N-methylenediacrylamide (N,N-MDAM) as a cross-linker and benzoyl peroxide (BPO) as an initiator. The molecularly imprinted membranes and the non-imprinted membranes were prepared using acetophenone(AOPH) and di octylphathalate(DOP)as plasticizers in PVC matrix. The slopes and detection limits of the liquid electrodes ranged from)-18.1,-17.72 (mV/decade and )4.0 x 10-
... Show MoreVitamin A, namely retinol is still the most proper agent for modulating so many biochemical reactions and biological functions in different tissues and organs. In addition to the provitamins A and α, βand γ-carotenoids that are present in various foods from either animal or plant origin, retinoids and rexinoids form the natural and synthetic analogs that are chemically related or unrelated and can be added as food supplements for deficiency disorders of vitamin A or used to alleviate or treat certain health problems such as skin carcinoma, acne, skin aging and dermatitis.
This work involves the preparation of high yield iminochalcon compounds (B1-B15) through two parts. The first part involves the preparation of 2,4-dihydroxy Chalcone (A1-A15) by the condensation of 2,4-dihydroxy acetophenone with aryl aldehyde in the presence of sodium hydroxide (40%) as a catalyst. The second part includes the preparation of iminochalcon from the condensation of p-hydroxy aniline with 2,4-dihydroxy chalcone derivatives )A1-A15) in the presence of some drops of conc. H2SO4. Thin-layer chromatography ((TLC) was used to control the chemical reaction . These new derivatives were characterized by using FT-IR and 1H-NMR spectroscopy. These synthesized
... Show MoreIn this work, the(m-phenylenediamine) and (2-naphthol) have been used in the synthesis of tetradentate ligand [m-phenylenedi(azo-2-naphthol)][H2L] type (N2O2). The ligand was refluxed in the ethanol with the metal ions [Co(II), Cu(II) and Zn(II)] salts, using triethyleamine as a base in (2:2) molar ratio to give the binuclear complexes. These complexes were characterised by (A.A), F.T.I.R, (U.V-Vis) spectroscopies, along with conductivity, chloride content and melting point measurement. These studies revealed an octahedral geometries for Co(II), Cu(II) and Zn(II) complexes with the general structure [M2(L)2(H2O)4]. The ligand and its complexes exhibited biological activity against the Bacillus(G+) strain and the
... Show More