The spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A promising approach to improve the cancer cell selectivity of methotrexate is the chemical transformation into reversible derivatives which convert the conjugate to the parent drug by virtue of enzyme within cancer tissue. The present study includes the synthesis of two derivatives of methotrexate which are :-Schiff base methotrexate-silibinin conjugate ( compound 5), and Methotrexate-silibinin conjugate (compound 6).The synthesis of the target compounds was accomplished following multistep reaction procedures. The chemical reactions were followed up and purity of the products was checked by TLC. The structures of the final compounds and their intermediates were characterized and identified by their melting points, infrared spectroscopy, 1H-NMR and elemental microanalysis(C H N S).The anticancer activity of these compounds was investigated by HEP-2 cell line(Larynx carcinoma), which showed that compounds 5 and 6 have the higher activity than methotrexate or silibinin alone.These are promising data for the discovery of new anticancer agents in future. These compounds may deliver the parent drug selectively into the cancer cells to be hydrolyzed by enzymes that are elevated in tumor tissues compared with normal tissues . Keywords: Methotrexate, Silibinin, Cancer treatment resistance, Folate receptor, Cancer cell targeting.
New Schiff base ligand (E)-6-(2-(4-(dimethylamino)benzylideneamino)-2-(4-hydroxyphenyl)acetamido)-3,3- dimethyl-7-oxo-4-thia-1- azabicyclo[3.2.0]heptane-2-carboxylic acid = (HL) was synthesized via condensation of Amoxicillin and 4(dimethylamino)benzaldehyde in methanol. Figure -1 Polydentate mixed ligand complexes were obtained from 1:1:2 molar ratio reactions with metal ions and HL, 2NA on reaction with MCl2 .nH2O salt yields complexes corresponding to the formulas [M(L)(NA)2Cl],where M=Fe(II),Co(II),Ni(II),Cu(II),and Zn(II), A=nicotinamide .
In this paper, an algorithm for binary codebook design has been used in vector quantization technique, which is used to improve the acceptability of the absolute moment block truncation coding (AMBTC) method. Vector quantization (VQ) method is used to compress the bitmap (the output proposed from the first method (AMBTC)). In this paper, the binary codebook can be engender for many images depending on randomly chosen to the code vectors from a set of binary images vectors, and this codebook is then used to compress all bitmaps of these images. The chosen of the bitmap of image in order to compress it by using this codebook based on the criterion of the average bitmap replacement error (ABPRE). This paper is suitable to reduce bit rates
... Show MoreIn this article, we design an optimal neural network based on new LM training algorithm. The traditional algorithm of LM required high memory, storage and computational overhead because of it required the updated of Hessian approximations in each iteration. The suggested design implemented to converts the original problem into a minimization problem using feed forward type to solve non-linear 3D - PDEs. Also, optimal design is obtained by computing the parameters of learning with highly precise. Examples are provided to portray the efficiency and applicability of this technique. Comparisons with other designs are also conducted to demonstrate the accuracy of the proposed design.
In this paper we proposes the philosophy of the Darwinian selection as synthesis method called Genetic algorithm ( GA ), and include new merit function with simple form then its uses in other works for designing one of the kinds of multilayer optical filters called high reflection mirror. Here we intend to investigate solutions for many practical problems. This work appears designed high reflection mirror that have good performance with reduction the number of layers, which can enable one to controlling the errors effect of the thickness layers on the final product, where in this work we can yield such a solution in a very shorter time by controlling the length of the chromosome and optimal genetic operators . Res
... Show MoreThe current research is concerned with studying the variables in the promotion process which influence the advertisement design structure, as the accomplished design and construction process is subject to many variables, whether they were intellectual or technological, internal or external variables. These variables may overlap in order to get a comprehensive system for the artistic configuration, that any design in its content reaches the highest levels of perfection is connected to the extent of its compliance with and approximation to these variables, that is why we find their reflections deeply rooted in the individual's mind, especially the designer artist who is influenced by everything surrounding him forming knowledge systems res
... Show MoreMassive multiple-input multiple-output (MaMi) systems have attracted much research attention during the last few years. This is because MaMi systems are able to achieve a remarkable improvement in data rate and thus meet the immensely ongoing traffic demands required by the future wireless networks. To date, the downlink training sequence (DTS) for the frequency division duplex (FDD) MaMi communications systems have been designed based on the idealistic assumption of white noise environments. However, it is essential and more practical to consider the colored noise environments when designing an efficient DTS for channel estimation. To this end, this paper proposes a new DTS design by exploring the joint use of spatial channel and n
... Show Moresensor sampling rate (SSR) may be an effective and crucial field in networked control systems. Changing sensor sampling period after designing the networked control system is a critical matter for the stability of the system. In this article, a wireless networked control system with multi-rate sensor sampling is proposed to control the temperature of a multi-zone greenhouse. Here, a behavior based Mamdany fuzzy system is used in three approaches, first is to design the fuzzy temperature controller, second is to design a fuzzy gain selector and third is to design a fuzzy error handler. The main approach of the control system design is to control the input gain of the fuzzy temperature controller depending on the cur
... Show MoreThe aim of this paper is to design feed forward neural network to determine the effects of
cold pills and cascades from simulation the problem to system of first order initial value
problem. This problem is typical of the many models of the passage of medication throughout
the body. Designer model is an important part of the process by which dosage levels are set.
A critical factor is the need to keep the levels of medication high enough to be effective, but
not so high that they are dangerous.
A perturbed linear system with property of strong observability ensures that there is a sliding mode observer to estimate the unknown form inputs together with states estimation. In the case of the electro-hydraulic system with piston position measured output, the above property is not met. In this paper, the output and its derivatives estimation were used to build a dynamic structure that satisfy the condition of strongly observable. A high order sliding mode observer (HOSMO) was used to estimate both the resulting unknown perturbation term and the output derivatives. Thereafter with one signal from the whole system (piton position), the piston position make tracking to desire one with a simple linear output feedback controller after ca
... Show MoreThe reaction of 2-amino-benzothiazole with bis [O,O-2,3,O,O – 5,6 – (chloro(carboxylic) methiylidene) ] – L – ascorbic acid (L-AsCl2) gave new product 3-(Benzo[d]Thaizole-2-Yl) – 9-Oxo-6,7,7a,9-Tertrahydro-2H-2,10:4,7-Diepoxyfuro [3,2-f][1,5,3] Dioxazonine – 2,4 (3H) – Dicarboxylic Acid, Hydro-chloride (L-as-am)), which has been insulated and identified by (C, H, N) elemental microanalysis (Ft-IR),(U.v–vis), mass spectroscopy and H-NMR techniques. The (L-as am) ligand complexes were obtained by the reaction of (L-as-am) with [M(II) = Co,Ni,Cu, and Zn] metal ions. The synthesized complexes are characterized by Uv–Visible (Ft –IR), mass spectroscopy molar ratio, molar conductivity, and Magnetic susceptibility techniques. (
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