In the course of generating a library of open-chain epothilones, we discovered a new class of small molecule anticancer agents that has no effect on tubulin but instead kills selected cancer cell lines by harnessing reactive oxygen species in an iron-dependent manner.
A series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed struct
... Show More4-chloro and 4- nitro substituted phenol and aniline incorporated to a carboxylic group of naproxen a well-known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of these compounds (I-IV) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (2.5 mg/Kg) of naproxen. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compounds I and IV might show higher effect comparable to that of naproxen and to that of compounds II & III whic
... Show MoreThis study includes design and synthesis of new non-steroidal anti-inflammatory agents (NSAIDs) with expected cyclooxygenase-2 (COX-2) selective inhibition to achieve better activity and low gastric side effects. Two series of compounds have been designed and synthesized as potential NSAIDs,these are: Salicylamide derivatives (compounds 3,4,5 ) and Diflunisal derivatives (compounds 10&11). In vivo acute anti-inflammatory effect of one of the synthesized agents (compound 3) was evaluated in the rat using egg-white induced paw edema model of inflammation. Preliminary pharmacological study revealed that compound 3 exhibited less anti-inflammatory effect compared to that of aspirin after
... Show MoreA group of amino derivatives [4-aminobenzenesulfonamide,4-amino-N¹ methylbenzenesulfonamide, or N¹-(4-aminophenylsulfonyl)acetamide] bound to carboxyl group of mefenamic acid a well known nonsteroidal anti-inflammatory drugs (NSAIDs) were designed and synthesized for evaluation as a potential anti-inflammatory agent. In vivo acute anti-inflammatory activity of the final compounds (9, 10 and 11) was evaluated in rat using egg-white induced edema model of inflammation in a dose equivalent to (7.5mg/Kg) of mefenamic acid. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-amino-N-methylbenzenesulfonamide derivative (c
... Show MoreFood fortification has an important and necessary role in compensating for the shortage of nutritional micronutrients, especially in developing and least developed countries. So, 12 samples of flour available in the local market, whether imported or locally produced flour, were obtained during 2019. The amount of base metal of the necessary iron element in the flour models studied which are available in local markets, measured by spot testing and was compared with the values that should be added according to the specification Iraqi standard. Results revealed the qualitative evaluation of iron in locally produced flour does not conform to the Iraqi standard and is almost free of any reinforcement. While the percentage of imp
... Show MoreThis research aims to determine the concentration of radionuclides in dust samples on the public streets of the small side of Diwaniyah city in Iraq as a result of movements of wheels and cars using the gamma spectra and high purity germanium detector (HPGe) with resolution of (2.3 keV) for energy (1.332 MeV) of cobalt 60Co. Dust samples were collected from the streets Diwaniyah city with (26) samples prepared for measurement. The results of the specific activity concentration of Uranium-238, Thorium-232, Potassium-40 and Cesium-137 were (14.66 ± 0.950, 26.29 ± 2.431, 219.04 ± 15.150 and 11.49 ± 0.876) Bq/kg respectively. The radiation parameters Rae
This study synthesized polyacetal from the reaction of polyvinyl alcohol with para-nitrobenzaldehyde. Polyacetal/polyvinylpyrrolidone polymer blends were prepared using solution casting. Gold nanoparticles (AuNPs) and silver nanoparticles (AgNPs) were biosynthesized using onion peel extract as the reducing agent. Nanocomposites were fabricated by blending polyacetal/PVP with AuNPs and AgNPs at different ratios. XRD and FESEM characterized the AuNPs and AgNPs. FTIR, FESEM, TGA, and DSC characterized the polyacetal, polymer blends, and nanocomposites. DSC and TGA confirmed the improved thermal stability of the polymer blends and nanocomposites. Nanocomposites demonstrated higher efficacy in inhibiting lung cancer cell lines compared t
... Show MoreThe Mannich base ligand was synthesized in an ethanol medium through a condensation reaction of 2-mercaptobenzimidazole and ciprofloxacin at room temperature. Subsequently, several metal complexes of this ligand were prepared. To characterize both the base ligand and the metal complexes, various techniques were employed, including elemental analysis, FT-IR spectroscopy, UV-Vis spectroscopy, molar conductivity measurements, magnetic moment determination, and melting point analysis. The results were shown that the metal complexes formed have the formula [Cr(L)2Cl2] Cl.H2O and [Rh(L)2(H2O)2] Cl3.H2O, where L= mannich base ligand. Based on spectroscopic analytical, coordination with metal ions involves the 'N' donor atom of mannich base
... Show MoreFive novel nickel, iron, cobalt, copper, and mercury complexes were synthesized from tetraazamacrocyclic Schiff base ligand (L), which were derived from 3-(4-(dimethyl amino) benzylidene) pentane-2,4-dione and 1,2- diaminocyclohexane in a 2:2 molar ratio. Many physico-chemical and spectroscopic techniques, including melting point, 1HNMR, 13CNMR, elemental analysis, molar conductance, magnetic susceptibility, UV-Vis, FT-IR, and thermogravimetric analysis (TGA), were used to characterize the Schiff base ligand and all metal complexes. The octahedral geometry of all the complexes [MLCl2] is confirmed by spectroscopic analyses. All substances' biological properties, such as their in vitro antioxidant activity or level of free radical scavenging
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