Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenocarcinoma and mouse hepatoblastoma cells with low cytotoxic effect against normal human breast cells. Their binding mode to the active site of several histone deacetylases has been studied by docking and the results gave a preliminary indication that they could be successful histone deacetylase inhibitors.
The reaction of 2-amino benzoic acid with 1,2-dichloroethane under reflux in methanol and KOH as a base to gave the precursor [H4L]. The precursor under reflux and drops of CH3COOH which reacted with (2mole) from salicycaldehyde in methanol to gave a new type N2O4 ligand [H2L], this ligand was reacted with (MCl2) Where [M= Co (II), Ni(II), Cu(II) and Zn(II)] in (1:1) ratio at reflux in methanol using KOH as a base, to give complexes of the general formula [M(L)]. All compounds have been characterized by spectroscopic methods [1H NMR ( just to the ligand), FTIR, uv-vis, atomic absorption], melting point, conductivity, chloride content, as well as magnetic susceptibility measurements. From the above data, the proposed molecular structu
... Show MoreThe reaction of 2-amino benzoic acid with 1,2-dichloroethane under reflux in methanol and KOH as a base to gave the precursor [H4L]. The precursor under reflux and drops of CH3COOH which reacted with (2mole) from salicycaldehyde in methanol to gave a new type N2O4 ligand [H2L], this ligand was reacted with (MCl2) Where [M= Co (II), Ni(II), Cu(II) and Zn(II)] in (1:1) ratio at reflux in methanol using KOH as a base, to give complexes of the general formula [M(L)]. All compounds have been characterized by spectroscopic methods [1H NMR ( just to the ligand), FTIR, uv-vis, atomic absorption], melting point, conductivity, chloride content, as well as m
... Show MoreABSTRACT : This research involves the synthesis of five to seven heterocyclic compounds starting with Schiff’s bases which derived from oxime as a starting material. 1.3-oxazepine derivatives were prepared from adding different anhydrides to the Schiff bases, tetrazole and thiazolidinone derivatives synthesized from add sodium azide and thioglycolic acid to the same Schiff’s bases as a five members ring. Pyrimidine derivatives were prepared after the reaction of the azomethine group with acetyl chloride and then urea and thiourea to synthesis on derivatives contain the six members ring. Another step included identified and confirmed these compounds by FT- IR, 1HNMR, TLC and 13CNMR finally, step included the assay of biological activity
... Show Morethe traumatic memory of their ancestors. The novel navigates sites of trauma, memory, and blues music while resisting the bourgeoisie-capitalist relationships that permeated not only white society but also African American communities. Jones’s novel presents the plight of an African American woman, Ursa, caught between the memory of her enslaved foremothers and her life in an emancipated world. The physical and spiritual exploitation of African American women who bear witness to the history of slavery in Corregidora materializes black women’s individuality. This article is framed by trauma studies as well as the Marxists’ concepts of commodification, accumulation, and production. Ursa, one of the Corregidora women, represents
... Show MoreThis study is attempt to improve thermal isolation through measuring thermal conductivity composite of on polyester resin with fillers of (TiO2, ZnO, Acrylonitril, wood flour Coconut (Wf). The grain size of the fillers is 200 µm. The number of samples is (16) in addition to the virgin sample; these samples are prepared by cast molding method for polyester with filler volume fractions (5%, 10%, 15% and 20%). Shore hardness tests were used to measure the hardness and Lee disk method for thermal conductivity. The experimental results showed that the (20% ZnO) sample has the maximum value of thermal conductivity where (20% w.f) has minimum thermal conductivity .on the other hand (15% ZnO) sample give the maximum value of hardness where (20% w
... Show MoreTechnique was used to retail for analyzing atom beryllium ion cathode of an atom lithium to six pairs of functions wave which two ?????? and the rest of the casing moderation and to analyze atom lithium ion Mob atom beryllium to three pairs of functions wave pair of casing and the rest of the casing moderation using function wave Hartree Fock and each casing email wascalculate expected values ??....
The goal of this investigation is to prepare zinc oxide (ZnO) nano-thin films by pulsed laser deposition (PLD) technique through Q-switching double frequency Nd:YAG laser (532 nm) wavelength, pulse frequency 6 Hz, and 300 mJ energy under vacuum conditions (10-3 torr) at room temperature. (ZnO) nano-thin films were deposited on glass substrates with different thickness of 300, 600 and 900 nm. ZnO films, were then annealed in air at a temperature of 500 °C for one hour. The results were compared with the researchers' previous theoretical study. The XRD analysis of ZnO nano-thin films indicated a hexagonal multi-crystalline wurtzite structure with preferential growth lines (100), (002), (101) for ZnO nano-thin films with different thi
... Show MoreHypertension is identified as one of the most significant risk factors for cardiovascular diseases (CVDs). There is growing evidence showing that oxidative stress plays a major role in hypertension. Increased production of reactive oxygen species and decrease bioavailability of antioxidant have been demonstrated in experimental and human hypertension. The present study was directed to determine the beneficial effect of the antioxidant vitamin C in patients with essential hypertension treated with the calcium channel blocker (amlodipine) or with the angiotensin converting enzyme inhibitor (enalapril). Ninety six patients (50 females and 46 males) with essential hyp
... Show MoreAlopecia areata is considered as a major health problem, its importance is attributed to its
recent increased incidence in our population. Till now, there is no exact cause for alopecia areata
although researchers thought it's an autoimmune disease.
This clinical study was designed to evaluate the role of trace elements (zinc and copper) in patients
with alopecia areata. Twenty patients were diagnosed as having alopecia areata with an age range
(10-40 years) were involved in this study. Normal subjects of the same age group were also
evaluated as control. The level of serum Zn and Cu were measured by flame atomic absorption
spectrophotometry in both control and patient group. And the ratio of Zn/Cu was also estimated