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 series of lanthanide metal (???) complexes have been prepared from the new azo ligand, 3-(1-methyl-2-benzimidazolylazo)-Tyrosine (MBT). The structural feature were confirmed on the basis of their elemental analysis, metal content, molar conductance, magnetic measurement, FTIR, 1 HNMR and UV-Vis spectra studies. The isolated complexes were found to have a mole ratio (1:2) (metal:ligand) stoichiometry with the general formula [Ln(MBT)2]Cl (Ln(???) = La, Ce, Pr, Nd, Sm, Eu and Gd). The chelates were found to have octahedral structures. The FTIR spectra shows that the ligand (MBT) is coordinated to lanthanide ions as a N, N, O-tridentate anion via benzimidazole nitrogen, azo nitrogen and oxygen of hydroxyl after deprotonation. Com
... Show Morenew, simple and fast solid-phase extraction method for separation and preconcentration of trace theophylline in aqueous solutions was developed using magnetite nanoparticles (MIONPs) coated with aluminium oxide (AMIONPs) and modified with palmitate (P) as an extractor (P@AMIONPs). It has shown that the developed method has a fast absorbent rate of the theophylline at room temperature. The parameters that affect the absorbent of theophylline in the aqueous solutions have been investigated such as the amount of magnetite nanoparticle, pH, standing time and the volume, concentration of desorption solution. The linear range, limit of quantification (LOQ) and limit of detection (LOD) for the determination of theophylline were 0.05-2.450 μg mL-
... Show MoreAn International Publisher for Academic and Scientific Journals The mucilage of white and black chia seeds were extracted and determining their contents of bioactive compounds such as tannins, glycosides, flavonoids, phenols, and studying their activity as anti-filamentary and anticancer. Results showed that tannins exist in white chia seeds with 35%while it is 38% in black seeds, flavonoids represent 0.98mg/ml in white chia seeds and 1.5 mg/ml for black seeds. Both kinds of seeds showed anti-filamentaryactivity, the inhibition ratio was 86.5% for white seeds and 97.3% for black seeds. Chia black seeds showed anticancer activity and the inhibition of the tumor muscle cell line ratio (GI%) was 34.8% at 50mg/ml concentration and 88.4%
... Show MoreIn spite of increasing clinical cases which caused by enteroviruses transferred by water and no documents about entericviruses in the Iraqi water standards. The use of coliphages as an indicator of enteroviruses and fecal pollution were suggested two procedures were applied . The first is Two-Step Enrichment Method and the second is Single Agar Layer Method. Both methods gives good results in Identification of coliphages through testing fifty different water samples (Tap water, Surface water and Bottled water) the study shows the presence of coliphages in fourteen samples.
Abstract
Itraconazole is a triazole antifungal given orally for the treatment of oropharyngeal and vulvovaginal candidiasis, for systemic infections including aspergillosis, candidiasis, and for the prophylaxis of fungal infections in immunocompromised patients.
The study aimed to formulate a practical water-insoluble Itraconazole, with insufficient bioavailability as nanosuspension to increase aqueous solubility and improve its dissolution and oral bioavailability.
Itraconazole nanosuspension was produced by a
... Show MoreBladder cancer (BC) is the predominant malignant neoplasm in the urinary system and ranks as the tenth most prevalent malignant tumor worldwide. Compared with females, males displayed a four-fold more common incidence of bladder cancer. It mainly affects men. Bladder cancer is the fourth most prevalent neoplasm in males. The most important protein that makes up high density lipoprotein (HDL), ApoA-I apolipoprotein A1 is essential in regulating the right amount of cholesterol. Multiple inquiries have demonstrated that APOA1 plays a pivotal role in the progression, infiltration, and spread of tumors. Objectives. The objective of this study was to measure the level of urine to serum apolipoprotein A1 in patients suffering from bladder
... Show MoreThis paper signifies the contradictory point of view in John Clare’s poetry. Clare (1794-1864) is an English romantic poetry in the nineteenth century, who writes more than ten volumes about nature. So, this study highlights the concept of Psychoanalytic theory which is ‘ambivalence’ and how through this theory can interpret any literary text on the basis of utilizing psychoanalytic methods to literary texts in order to reveal the author's inner emotions such as motives, dreams, as well as wishes. Consequently, the concept of ‘ambivalence’ has a lot in common with the human psyche and its struggles. Sometimes the reader finds the author/poet talking about something real or a notion with pleasant sentiments
... Show MoreIt is more beneficial science and created and the highest honor is the Koran Sciences, God has honored research in this fun science, came this research that shed the light on the radical incision, and Naughty derivatives as contained in the Koran, and illustrate the diversity of Saghma morphological, and fork them from derivatives what it entailed connotations, as well as the evacuation of cryptic in some of these verses from the biological secrets take minds newly exposed Anitrjt science under the name of scientific miracles.
The research methodology is revenue verse which included the word, and revenue lexical meaning and its meaning in the context of the Qur'an, and reflect the views of the commentators of the verse, and then the r
In this study, new heterocyclic compounds were synthesized through the cyclization reactions of o-phenylenediamine (1) with various organic reagents. Benzodiazepine derivatives (2-4) were obtained by reaction of (1) with ethylacetoacetate, malonic acid and acetyl acetone.Treatment of compound (1) with chloroacetamide, chloroacetic acid, p-bromophenacyl bromide and oxalic acid dihydrate afforded quinoxaline derivatives (5-8), respectively. Reaction of compound (1) with benzoic acid, piperonal, cyclohexanone and carbon disulfide resulted in the formation of compounds (9-12), respectively. Finally, reaction of compound (12) with chloroacetic acid in the presence of potassium hydroxide produced compound (13).