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.
All new compounds synthesized by many reactions starting from a product the compounds [I]a,b from reaction of 3-phenylenediamine or 4-phenylenediamine with chloroacetyl chloride, then the compounds [I]a,b reacted with potassium thiocyanate to yield compounds [II]a,b. While the compounds[III]a,b yield from reacted the compounds [I]a,b with sodium azide then the compounds [III]a,b reacted 1,3-dipolar cycloaddition reaction with acrylic acid to give compounds [IV]a,b and the later compounds reacted with phenylene diamine to product benzimidazole compounds [V]a,b . In addition to synthesized acid chloride compounds [VI]a,b by reacted the compounds [IV]a,b with thionyl chloride .Finally reacted the compounds [VI]a,b with different aromatic amine
... Show MoreAsthma is a chronic respiratory disorder of airways characterized by inflammation, hyperresponsiveness, inflammatory cell infiltration, mucous secretion, and remodelling. Ammi majus is medicinal plant belong to family of Apiaceous which has anti-inflammatory and antioxidant activities. This study designed to investigate of anti-asthmatic activity of alcoholic extract of Ammi majus in improvement of asthma. Forty-eight healthy female mice divided to six groups Group I: the negative control group (distal water only), Group II: Positive control group (ovalbumin group), Group III: Ammi majus (64 mg/kg/day) with sensitization, Group IV:Ammi majus (128 mg/kg/day) with sensitization, Group V: Ammi majus (64 mg/kg/day) without sensitiza
... Show MoreAsthma is a chronic respiratory disorder of airways characterized by inflammation, hyperresponsiveness, inflammatory cell infiltration, mucous secretion, and remodelling. Ammi majus is medicinal plant belong to family of Apiaceous which has anti-inflammatory and antioxidant activities. This study designed to investigate of anti-asthmatic activity of alcoholic extract of Ammi majus in improvement of asthma. Forty-eight healthy female mice divided to six groups Group I: the negative control group (distal water only), Group II: Positive control group (ovalbumin group), Group III: Ammi majus (64 mg/kg/day) with sensitization, Group IV:Ammi majus (128 mg/kg/day) w
... Show MoreCardiac toxicity can occur during the therapy with several cytotoxic drugs, including 5- Fluorouracil (5- FU). It is an antimetabolite that acts during the S phase of the cell cycle and is activated by thymidine phosphorylase into fluorodeoxyuridylate (5 fluoro 2'deoxyuridine 5'monophosphate, 5-FdUMP) that inhibits thymidylate synthase, thus preventing DNA synthesis that leads to imbalanced cell growth and ultimately cell death. It is still a widely used anticancer drug, since 1957. The present study aimed to evaluate the possible cardio-protective effects of ethanolic artichoke extract (Cynara scolymus L.) against 5-fluorouracil (5-FU) induced cardio-toxicity in rats by evaluating serum levels of Alanine aminotransferase, aspartate amin
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Playing is the only common language among children in every place and time, to the fact that what distinguishes the children is their quest to play and fun way innate, not acquired, which is expressed with the child really is one of the rights. And play a key entrance to the growth of the child mentally, intellectually and cognitively and not for the child emotionally and socially just. In the play the child begins to identify and classify objects and learn concepts and circulate among themselves on a linguistic basis. Activity here and play a major role in leading the linguistic development of the child in the composition has the communication skills.
The Games (especially intellectual ones) Whatever the cause of the development
... Show MoreMagneto-rheological (MR) Valve is one of the devices generally used to control the speed of Hydraulic actuator using MR fluid. The performance of valve depends on the magnetic circuit design. Present study deals with a new design of MR valve. The finite element analysis is carried out on this valve to optimize its design. The design of the magnetic circuit is accomplished by magnetic finite element software such as Finite Element Method Magnetic (FEMM). The Model dimensions of MR valve, material properties and the circuit properties of valve coil are taken into account. The results of analysis are presented in terms of magnetic strength and magnetic flux density. The valve can be operated with variable flow rate by varying the current. It i
... Show MoreResearch is a study conducted by a researcher or a group of researchers to uncover ambiguity, complete a knowledge, or define a relationship, Solve a problem, or answer a question by carefully investigating the comprehensive and in-depth examination of the evidence and evidence related to this knowledge, revealing a relationship, or solving a problem, or answering a question, to be a systematic, In evidence and evidence that reveal facts and general rules, relationships or solutions, in addition to providing knowledge Human rights are verifiable, tested and confirmed. The university research (graduate research, master's thesis, doctoral dissertation) is the most important type of research, and it is supposed to be the best one, since it
... Show MoreIn this work, the design and implementation of a smart energy metering system has been developed. This system consists of two parts: billing center and a set of distributed smart energy meters. The function of smart energy meter is measuring and calculating the cost of consumed energy according to a multi-tariff scheme. This can be effectively solving the problem of stressing the electrical grid and rising consumer awareness. Moreover, smart energy meter decreases technical losses by improving power factor. The function of the billing center is to issue a consumer bill and contributes in locating the irregularities on the electrical grid (non-technical losses). Moreover, it sends the switch off command in case of the consumer bill is not
... Show MoreIn this paper, a single-phase boost type ac-dc converter with power factor correction (PFC) technique is designed and implemented. A current mode control at a constant switching frequency is used as a control strategy for PFC converter. The PFC converter is a single-stage singleswitch boost converter that uses a current shaping technique to reshape the non-sinusoidal input current drawn by the bulky capacitor in the conventional rectifier. This technique should provide an input current with almost free-harmonics, comply with the IEC61000-3-2 limits, and a system operates with near unity power factor. The other function of the boost converter that should be
accomplished is to provide a regulated DC output voltage. The complete designed