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.
In this study, the effect of grafting with magnesium (Mg) ratios (0.1, 0.3, 0.5) on the structural and optical properties of cadmium oxide films (CdO) was studied, as these films were prepared on glass bases using the method of pulse laser deposition (PLD). The crystallization nature of the prepared membranes was examined by X-ray diffraction technique (XRD), which showed that the synthesis of the prepared membranes is polycrystalline, and (AFM) images also showed that the increased deformation with magnesium led to an increase in the grain size ratio and a decrease in surface roughness, as well as the absorption coefficient was calculated. And the optical energy gap for the prepared membranes, where it was found that the absorption coef
... Show MoreThe present study attempts to shed light on some biological aspects and characteristics of Piaractus brachypomus, including some biometrics, phenotypic and feeding pattern that characterizes this species. Besides, the study touches upon the body shape and the Otolith. These fish species have recently been seen frozen in the Iraqi local market. The standard length of fish specimens in this study reach 26.55cm it exceeded the specimens of Pacu fish collected from other studies from other countries, As well the specimens weight was 632gm it exceeded other studies mentioned in this manuscript. As the irregularity in the distribution of teeth rows, especially in the lower jaw was clear in our specimens. The average weight of some skull b
... Show MoreMercury-lead-antimony based superconductors with the formula Hg0.5 Pb0.5xSbxBa2Ca2Cu3O8+δ (x=0, 0.10 and 0.15) have been prepared by useing three step solid state reaction processes. Electrical resistivity, using four probe technique, is used to find the transition temperature Tc. It is found from that sample Hg0.5 Pb0.5Ba2Ca2Cu3O8.437 is semiconductor , sample Hg0.5 Pb0.4Sb0.1Ba2Ca2Cu3O8.353 is normal state with metallic behaviors, while sample Hg0.5 Pb0.35Sb0.15Ba2Ca2Cu3O8.233 is superconducting state with critical transition temperature (Tc) is 126K. X-ray diffraction (XRD) analysis showed a tetragonal structure with decrease in the c-axis lattice constant for the samples doped with Sb as compared with these which have no Sb
... Show MoreChukar partridge Alectoris chukar (Gray, 1830) is the only species of the 46 species of the genus Alectoris to be found in Iraq. At least there are fourteen subspecies of chukar were described from east Europe, the Middle East and west Asia, two of them were known to be found in Iraq, A.c. Kurdestanica (Meinertzhagen, 1923) from Alpine bio-geographical zone of altitude more than 2000m high, and A.c. werae Zarundny and Loudon, 1904, from the foothills of altitude not more than 400m. In between these two regions, there is another bio-geographical region known as the Irano-toranian zone 400-2000m high. Using morphological, ecological, behavioural, reproduction and hybridization criteria this study discove
... Show MoreIn this study, graphene oxide (GO) and reduced graphene oxide were synthesized by pulsed Nd:YAG laser with a fundamental wavelength (1064 nm) focused on the pure graphite target which was immersed in distilled water. Different pulse energies were applied in two cases; with and without magnetic field. The synthesized GO and rGO nanoparticles were characterized by UV-visible spectroscopy, X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy and atomic force microscopy (AFM) with and without magnetic field. The data show the presence of a magnetic field which illustrated increasing oxygen functional groups of GO. This caused a change in the morphology of the surface of GO, increasing crystallite size from 12.19 nm to 71.2
... Show MoreThe snthesis and characterization of cobalt(II), nickel(II), copper(II) and zinc(II) complexes of azo ligand 4-[(5-acetyl-2-aminophenyl)- diazenyl]-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one derived from 4-aminoantipyrine and 4-aminoacetophenone are reported. The nature of the compounds have been studied followed by mole ratio and methods of continuous contrast, Beer′s law followed during a condensation rate (1 × 10-4 – 3 × 10-4 M). The analytical data showed that all the complexes are in 1:2 metal-ligand ratio. An octahedral geometry have been suggested for all the compounds and biological studies of all the complexes were evaluated against different types of antimicrobial strains.
The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (5-8). These compounds were characterized spectroscopically by
... Show MoreThe purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (
This research includes the synthesis of some new N-Aroyl-N \ -Aryl thiourea derivatives namely: N-benzoyl-N \ -(p-aminophenyl) thiourea (STU1), N-benzoyl-N \ -(thiazole) thiourea (STU2), N-acetyl-N ` -(dibenzyl) thiourea (STU3). The series substituted thiourea derivatives were prepared from reaction of acids with thionyl chloride then treating the resulted with potassium thiocyanate to affored the corresponding N-Aroyl isothiocyanates which direct reaction with primary and secondary aryl amines, The purity of the synthesized compounds were checked by measuring the melting point and Thin Layer Chromatography (TLC) and their structure, were identified by spectral methods [FTIR,1H-NMR and 13C-NMR].These compounds were investigated as a
... Show MoreThe dangers of (Israel's) integration with Arab countries in the middle east region will threaten the Arab security structure dimension, which the latter makes the Arab regional system vulnerable for distortion due to its nominal and symbolic value which is far from the Arab self and questioning with its effectiveness in comparing with the real capabilities to Arab countries in achieving the common targets. So, how to assess the different problems that began to hit the structure of the Arab regional system? and how to pledge an allegiance after putting forward what is known as the American Deal of the Century for the administration of former US President Donald Trump for making another step toward normalization with (Israel)?. The reveal
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