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 new ligand [N-(4-nitrobenzoylamino)-thioxomethyl] phenylalanine is synthesized by reaction of 4-nitrobenzoyl isothiocyanate with phenylalanine (1:1). It is characterized by micro elemental analysis (C.H.N.S.), FT-IR, (UV-Vis) and 1H and 13CNMR spectra. Some metals ions complexes of this ligand were prepared and characterized by FT-IR, UV-Visible spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From results obtained, the following formula [M(NBA)2] where M2+ = Mn, Co, Ni, Cu, Zn, Pd, Cd and Hg, the proposed molecular structure for these complexes as tetrahedral geometry, except copper and palladium complexes are have square planer geometry.
The ligand 2-Hydroxy-N-pyridin-2-ylmethyl-acetamide(L) has been prepared from reaction of 2-(aminomethyl)pyridin with chloroacetic acid (1:1).It has been characterized by elemental analysis (C,H,N) ,'H, 13 C-NMR, IR and electronic spectra. The complexes of divalent (Co,Ni,Cu,Zn,Cd and Hg) ions and trivalent(Cr) ion have been synthesized and characterized by IR, electronic spectra, molar conductivity, atomic absorption and molar ratio (Ni 2+) complex. The analytical studies for the complexes show; octahedral for (Cr 3+),square planar for (Cu 2+) and (Co,Ni Zn, Cd and Hg) tetrahedral geometries. The study of biological activity of the ligand (L) and its complexes (Co,Ni,Cu,Cd,Hg) in two deferent concentration (1and5) mg/ml showed various acti
... Show MoreAt the beginning of the twentieth century distorting handling totalitarian phenomena of art, which can be called the stage of the test, transition from the theory of ideal theory and other realistic is not cushy, since it requires vision and reading and other concepts, and in light of this dialectic manifested research problem by asking the following Is affected by the design idealism and realism. Through the above mentioned questions, the researcher found rationale for addressing this problem, the study through his research, which is marked (idealism and realism in a comparative study design). And demonstrated the importance of research in the identification of the concept and the effectiveness of the two theories idealism and realism a
... 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 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 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
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