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.
Non-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphon
... Show MoreENGLISH
In 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.
The current study included, studying the ability of eight genera of plants belong to Brassicaceae family, Brassica tournifortii, Cakile Arabica, Capsella bursa – pastoris,Carrichtera annua, Diplotaxis acris, Diplotaxis haru , Eruca sativa and Erucaria hispanica to accumulate ten heavy metals Cadmium, Chromium , Copper, Mercury, Manganese ,Nickel ,Lead ,and Zinc . Plant leaves samples were collected from Al-Tib area during spring of 2021.The data demonstrated that, the highest conc. of Cd was 2.7 mg/kg in Diplotaxis acris leaves and lower value was 0.3 mg/kg in Cakile Arabica leaves. For Co, the highest conc.was 1.3 mg/kg in Capsella bursa – pastoris leaves, whereas the lower value was 0.5 mg/kg in Cakile arabica leaves. As for Cr ele
... Show MoreFind cares studying ways in the development of industrial products and designs: the way the progressive development (how typical) and root development (jump design), was the aim of the research: to determine the effectiveness of the pattern and the jump in the development of designs and industrial products. After a process of analysis of a sample of research and two models of contemporary household electrical appliances, it was reached a set of findings and conclusions including:1-leaping designs changed a lot of entrenched perceptions of the user on how the product works and its use and the size and shape of the product, revealing him about the possibilities of sophisticated relationships with the product, while keeping the typical desi
... Show MoreBackground: Malignant lymphoma is a term that describes primary tumors of the lymphoreticular system, almost all of which arise from lymphocytes.MMP-1 is the most ubiquitously expressed interstitial collagenase, a subfamily of MMPs that cleaves stromal collagens. It is also called collagenase-1.TIMPs which inhibits MMP activity and thereby restrict extracellular matrix breakdown, TIMP-1 is a stromal factor that has a wide spectrum of functions in different tissues. Material and Methods: This study was performed on (68) formalin-fixed, paraffin-embedded blocks, histopathologically diagnosed as lymphoma (head and neck lesions). Immunohistochemical staining of MMP1and TIMP1 was performed on each case of the study sample. Results: The expressio
... Show MoreAir pollution is one of the important problems facing Iraq. Air pollution is the result of uncontrolled emissions from factories, car exhaust electric generators, and oil refineries and often reaches unacceptable limits by international standards. These pollutants can greatly affect human health and regular population activities. For this reason, there is an urgent need for effective devices to monitor the molecular concentration of air pollutants in cities and urban areas. In this research, an optical system has been built consisting of aHelium-Neonlaser,5mWand at 632.8 nm, a glass cell with a defined size, and a power meter(Gentec-E-model: uno) where a scattering of the laser beam occurs due to air pollution. Two pollutants were examin
... Show MoreThis paper considers a new Double Integral transform called Double Sumudu-Elzaki transform DSET. The combining of the DSET with a semi-analytical method, namely the variational iteration method DSETVIM, to arrive numerical solution of nonlinear PDEs of Fractional Order derivatives. The proposed dual method property decreases the number of calculations required, so combining these two methods leads to calculating the solution's speed. The suggested technique is tested on four problems. The results demonstrated that solving these types of equations using the DSETVIM was more advantageous and efficient