Objective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the anticancer activities. Methods: Baclofen was initially reacted with aromatic aldehydes to create Schiff base derivatives (Ia–Ib), which were then closed in the next step using anhydrous acids to form oxazepine derivatives (IIa–IId). Results: The title compounds were synthesized successfully and identified using FT-IR, 1H NMR, and 13C NMR spectroscopy. Additionally, compound (IIc)’s (3-(4-chloro-phenyl)-4-[2-(4nitro-phenyl)-4,7-dioxo-4,7-dihydro-[1,3] oxazepin-3-yl]butyric acid) anticancer activity was assessed using MTT assay against FTC-133 (thyroid cancer) compared with WRL-68 (normal cell line). Discussion: The results showed that the viability of the FTC-133 cell was found to be greatest at 12.5 g/mL (96.52 ± 0.70) and lowest at 400 g/mL (35.378 ± 5.07). The effect of compound (IIc) on the normalizing of the WRL-68 cell line resulted in an IC50 for 62.39 ϻg/mL. Conclusions: It has been found that the compound (IIc) has good efficiency against thyroid cancer (FTC-133).
Abstract
The present study aims to assess the knowledge, attitude, and experience of off-label prescribing practice among physicians in Baghdad city hospitals. This cross-sectional study was performed through the period from November 1st 2018 to March 2019 at 17 hospitals, a self-administered questionnaire was utilized to collect data from the physicians, and the targeted hospitals were randomly selected at different regions in Baghdad City area. Out of the 400 distributed questionnaires to the physicians, 383 of them were returned completed, 57.2% indicated that they were reasonably familiar with the term “off label drug”, 57.7% mentioned that the most common medical reasons for the prescribing o
... Show MoreSurvivin, a member of inhibitor of apoptosis family is increasingly used as a target for cancer therapy design because it has a key role in cell growth and inhibition of cell apoptosis. Also it can be used as a biomarker for targeting cancer because it is found in almost all cancer but not normal cells. Our strategy was to design (computationally) a molecule to be used as survivin inhibitor. This molecule was named lead10 and was used furthermore to find (virtually) existing drugs with a good survivin inhibition activity.
Acidity constants at 30co and 0.125 ionic strength have been determined for the Nitrogous bases of nucleic acid; cytocine, uarcil and thymine, and found to be 3.55 x10-19 , 1.44 x10 -19 and 7.24 x10 -20 respectively. Stability constants of these bases with Thorium and uranyl ions have been determined. Results showed that metal ions Thorium and uranyl ions behave as hard acids and the nitrogenum bases behave as Hard bases according to Pearson's definition .Hardness – softness parameters for these ligands were calculated ,stability constants of complexes with metal ions could be arranged as follows :- Cytosine > Uracil > Thymine .
In this work, prepared new ligand[3- (1H-indol-3-yl) -2- (3-(4- methoxybenzoyl)thiouereido) propanoic acid](MTP) has been synthesized by reaction of 4-Methoxybenzoyl isothiocyanate with tryptophane(1:1), The ligand was characterized by elemental microanalysis C.H.N.S, FT-IR, UV-Vis and 1H,13C NMR spectra, Some transition metals complexes of this ligand were prepared and characterized by FT-IR, UV-Vis spectra, conductivity measurements, magnetic susceptibility and atomic absorption, From obtained results the molecular formula of all prepared complexes were [M(MTP)2] (M+2 =Mn, Co, Ni, Cu, Zn, Cd and Hg), the proposed geometrical structure for all complexes were tetrahedral except copper complex has a square planer geometry around metallic ion
... Show MoreA new Schiff base ligand Bis-1,4-di[N-3-(2-hydroxy-1-amino)- acetophenonylidene] benzylidene [L] and its complexes with (Mn(II) ,Co(II) ,Ni(II and Cu(II)) were synthesized . The ligand was prepared in two steps. In the first step a solution of (terphthalaldehyde) in methanol reacts under reflux with (p-aminoacetophenone) to give an intermediate compound [1-[3-({4-[(3-Acetyl-phenylimino)-methyl]-benzylidene}-amino)-phenyl]- ethanone which reacts in the second step with (2-Amino-phenol) giving the mentioned ligand. The complexes were synthesized by addition the corresponding metal salt solution to the solution of the ligand in methanol under reflux in (1:1) metal to ligand ratio. On the basis of, molar conductance, I.R., UV-Vis, HPLC, chlorid
... Show MoreSpecialized banks provide their banking activities to their customers at interest rates that are determined according to the approved bank policy, which is almost similar to most or most banks. To satisfy the financial desires of customers and at the same time it is a source of the bank's profits, However, these banks have been introduced to new services that they provide with the funds of the Central Bank initiative launched at the beginning of (2016) to address the economic stagnation that befell the country due to the (financial security) crisis that the country faced in 2014. To put forward initiatives amounting to nearly (15) trillion dinars, which were put forward through private commercial and Islamic banks and specialized
... Show MoreSince the Internet has been more widely used and more people have access to multimedia content, copyright hacking, and piracy have risen. By the use of watermarking techniques, security, asset protection, and authentication have all been made possible. In this paper, a comparison between fragile and robust watermarking techniques has been presented to benefit them in recent studies to increase the level of security of critical media. A new technique has been suggested when adding an embedded value (129) to each pixel of the cover image and representing it as a key to thwart the attacker, increase security, rise imperceptibility, and make the system faster in detecting the tamper from unauthorized users. Using the two watermarking ty
... Show MoreNew metal ion complexes were synthesized with the general formula; K[PtLCl4], [ReLCl4] and K[ML(Cl)2] where M = Pd(II), Cd(II), Zn(II) and Hg(II), from the Azo ligand (HL) [2-Hydroxy-3-((5-mercapto-1,3,4-thiadiazol-2-yl)diazenyl)-1-naphth aldehyde] (HL) the ligand was synthesized from (2-hydroxy-1-naphthaldehyde) and (5-amino-1,3,4-thiadiazole-2-thiol). The ligand and its metal complexes are characterized by phisco- chemical spectroscopic techniques (FT.IR, UV-Vis and Mass spectra, elemental analysis, molar conductivity, Atomic Absorption, Chloride contain and magnetic susceptibility). The spectral data suggest that the (HL) behaves as a bidentate ligand in all complexes. These studies revealed tetrahedral geometries for all metal complexes
... Show MoreThe synthesis of ligands with N2S2 donor sets that include imine, an amide, thioether, thiolate moieties and their metal complexes were achieved. The new Schiff-base ligands; N-(2-((2,4-diphenyl-3-azabicyclo[3.3.1]nonan-9-ylidene)amino)ethyl)-2-((2-mercaptoethyl)thio)-acetamide (H2L1) and N-(2-((2,4-di-p-tolyl-3-azabicyclo[3.3.1]nonan-9-ylidene)amino)ethyl)-2-((2-mercaptoethyl)thio) acetamide (H2L2) were obtained from the reaction of amine precursors with 1,4-dithian-2-one in the presence of triethylamine as a base in the CHCl3 medium. Complexes of the general formula K2[M(Ln)Cl2], (where: M = Mn (II), Co(II) and Ni(II)) and [M(Ln)], (where: M = Cu(II), Zn(II) and Cd(II); n =1-2, expect [Cu(HL2)Cl]) were isolated. The entity of ligands and
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