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.
have suffered from deteriorating residential neighborhoods, poor economic, social and urban living conditions of the population and deteriorating the infrastructural and superior services. These problems were the secretions of these cities' rapid urbanization. Based on the principles of sustainable urban planning and in order to achieve adequate opportunities for the lives of the population and provide them with sustainable livelihoods, policies have emerged to upgrade along the lines of community participation and programmes to reform and develop those neighbourhoods, raise their efficiency and make them livable. Thus, the problem of research was identified "The absence of a comprehensive cognitive perception of the most prominent facto
... Show MoreWe described herein the synthesized and characterized of new bent and liner core compounds containing thiazolidin-4-one ring[XI-XIII] and [XIV-XVI] respectively. These compounds synthesized by sequence reactions starting from reaction resorcinol or hydroquinone with chloracetyl chloride to yield compounds [I] and [II] ,then the later compounds reactant with 4-hydroxybenzylaldehyde to product dialdehyde compounds [III] and [IV] .The Schiff bases compounds[V-VII] and [VIII-X] synthesized from reaction the compound [III] or [IV] with different aromatic amines, while the bent and liner core mesogens containing thiazolidin-4-one ring [XI-XIII] and [XIV-XVI] synthesized from reaction Schiff bases compounds[V-VII] or [VIII-X] with thioglycolic aci
... Show MoreObjective: 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). Discus
... Show MoreThe study discussed here deals with the isolation of Aspergillus niger from palm dates, the formal and the most famous fruit in Iraq, to test and qualify this fungus isolate for its ability to produce citric acid. Submerged fermentation technique was used in the fermentation process. A.niger isolated from “Zahdi” Palme dates was used in the study of the fermentation kinetics to get the production efficiency of citric acid. Kinetics of CA production via fermentation by A. niger S11 was evaluated within 432 h fermentation time and under submerged conditions of 11% (w/v) sucrose, 5% (v/v) inoculum size, pH 4, 30 °C and 150 rpm. The maximum citric acid produced was (37.116 g/l). Kine
In this work, electrochemical process was presented to polymerized eugenol on Gr.2 and Gr.5 titanium alloys before and after treated by Micro Arc Oxidation (MAO), where Gr.2 is commercial pure titanium and Gr.5 is Ti-6Al-4V dental alloys. The deposited layers were characterized by scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDS), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR). The adhesion strength of polymeric thin-film was estimation by using pull-off adhesion test and the result was the adhesion strength of PE was (1.23 MPa) on Gr.2 before MAO and increase to (1.98 MPa) on Gr.2 after MAO treatment. The corrosion behavior of Gr.2 and Gr.5 alloy in artificial saliva environment at
... Show MoreThe term of heterocyclic chemistry focuses only on heterocyclic compounds, which consider as a percentage of organic chemistry, they equal to greater than sixty-five. These compounds are widely founded in nature and most of them are important to life. In the past few years, scientist fused on 1,2,4-triazoles and their condensed heterocyclic ring due to their medicinal significance, 1,2,4-triazole containing Sulphur atom is one of the important heterocyclic moieties due to its broad range of biological activities also their derivatives can accommodate one of the alternatives as electronic effect as exchanges of the electronic density (electron donating or withdrawing) groups ; for all what mentioned above they are consider as a core
... Show MoreUnter dem Titel " Technische Methoden im Fremdsprachunterricht als eine neueste Methode im Fremdsprachlernen, die Spiele als Muster"
versteht man, dass die Forschung sich mit einer neuen Methoden im Fremdsprachunterricht beschäftigt. Von den neuen Methoden im Unterricht sind die Spiele. So man sieht in den letzten Jahren viele Artikel zum Thema Spiele im Fremdsprschunterricht. Davon gehen wir aus, dass die Spiele im Unterricht eine groβe Rolle spielt, denn diese Methode macht Lust, Spaβ im Lernenprozeβ. Die Spiele im Unterricht bezeichnen als ein Mittel, um Unterricht etwas Schönes , Nützliches und Lebendigs zu sein. Die Spiele sind vielfälltig und unterscheidet sich nach den Themen und Materialien. In dieser F
... Show MoreBackground. In cases of spontaneous subarachnoid haemorrhage (SAH) with multiple intracranial aneurysms (MIAs) detected on angiography, some radiological clues assist in determining the site of a ruptured aneurysm which is bleeding is quite beneficial for the selection of the best treatment strategy. Case description. We report a case of a 60 years old patient who presented with spontaneous SAH, sellar hematoma, and three different aneurysms detected in angiography. Although the right Posterior communicating artery (PcomA) aneurysms showed Murphy’s teat on angiography intraoperatively, we discovered that the right superior hypophyseal aneurysm (SHA) was the source of the index bleeding. Both aneurysms were clipped successfully. Co
... Show MoreIn Indonesia, cattle feces (CF) and water hyacinth (WH) plants are abundant but have not been widely revealed. The use of microorganisms as decomposers in the fermentation process has not been widely applied, so researchers are interested in studying further. This study was to evaluate the effect of the combination of CF with WH on composting by applying white-rot fungal (WRF) (Ganoderma sp) microorganism as a decomposer. A number of six types of treatment compared to R1(ratio of CF:WH)(25%:75%)+WRF; R2(ratio of CF:WH)(50%:50%)+WRF; R3(ratio of CF:WH)(75%:25%)+WRF; R4(ratio of CF:WH)(25%:75%) without WRF; R5(ratio of CF:WH)(50%:50%) without WRF; R6(ratio of CF:WH)
... Show MoreABSTRACT: Oxadiazole ring is a heterocyclic molecule with an oxygen and two nitrogen atoms spread throughout its five-membered structure. There are four different isomers that have been discovered, Because of their wide applications in a range of sectors, including medications . Some of these biological activity are; anticonvulsant capacity, anticancer as well, antibacterial, antiviral, antifungal, antimalarial, antitubercular, anti-asthmatic, antidepressant, antidiabetic, antioxidant, antiparkinsonian, analgesic and anti-inflammatory, are just some of the therapeutic uses that have drawn attention to drug candidates containing an oxadiazole moiety. This review, we will examine the various methods of oxadiazole synthesis. The mo
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