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.
AA Noaimi, BM Fadheel, Saudi medical journal, 2008 - Cited by 25
The research has tackled about an important transformation within the whole region of middle east, especially there were more challenges which revealed under the huge pivotal interests of global powers that ruled the new world order by United states of America ; being very affected over the international and regional relations than any situations appeared previously within political realities. So that, many of variables inside the international scene which happened during of this period of contradicting strategic policies by the process of reforming and restructuring of difficult equations that imposed by international and regional allies and blocs . This article had concentrated over various strategic and political studies which reflect
... Show MoreWhen optimizing the performance of neural network-based chatbots, determining the optimizer is one of the most important aspects. Optimizers primarily control the adjustment of model parameters such as weight and bias to minimize a loss function during training. Adaptive optimizers such as ADAM have become a standard choice and are widely used for their invariant parameter updates' magnitudes concerning gradient scale variations, but often pose generalization problems. Alternatively, Stochastic Gradient Descent (SGD) with Momentum and the extension of ADAM, the ADAMW, offers several advantages. This study aims to compare and examine the effects of these optimizers on the chatbot CST dataset. The effectiveness of each optimizer is evaluat
... Show MoreThis research is carried out to investigate the behavior of self-compacting concrete (SCC) two-way slabs with central square opening under uniformly distributed loads. The experimental part of this research is based on casting and testing six SCC simply supported square slabs having the same dimentions and reinforcement. One of these slabs was cast without opening as a control slab. While, the other five slabs having opening ratios (OR) of 2.78%, 6.25%, 11.11%, 17.36% and 25.00%. From the experimental results it is found that the maximum percentage decrease in cracking and ultimate uniform loads were 31.82% and 12.17% compared to control slab for opening ratios (OR
... Show MoreSeveral adipokines are produced and secreted from adipose tissue, such as retinol binding protein-4, which triggers metabolic syndromes and insulin resistance. Retinol binding protein-4 transfers vitamin A or retinol in the blood. Higher levels of retinol binding protein-4 are interrelated with progress of metabolic disease, comprising obesity, metabolic syndrome, and type 2 diabetes mellitus. The present study investigates the role of retinol-binding protein-4 levels in type 2 diabetic Iraqi patients with metabolic syndrome. Sixty type 2 diabetic patients aged 40–53 years were examined. Of these 30 patients has metabolic syndrome and 30 without metabolic syndrome. The patients sampled were from the National Diabetes Center/ Mustansiriyah
... Show MoreDeconstruction is an intellectual stream that emerged as a result of the changes and requirements of the modern era. This stream extended from thought and literature to all arts, and the research included four chapters.
Chapter One: From the research, the research problem was identified in the form of a question: Have the ideas and deconstructive concepts represented in the abstract drawings of the artist Shaker Hassan Al Said?
The importance and limits of the research were reviewed and the goal of the research was to reveal the applications of ideas and deconstructive concepts in the abstract drawings of the artist Shaker Hassan Al Said, in addition to defining the most important terms contained in it.
Chapter Two: Previous
In this paper the concept of (m, n)- fully stable Banach Algebra-module relative to ideal (F − (m, n) − S − B − A-module relative to ideal) is introducing, we study some properties of F − (m, n) − S − B − A-module relative to ideal and another characterization is given