Preferred Language
Articles
/
nBeILZIBVTCNdQwCLqdz
New Niflumic Acid Derivatives as EGFR Inhibitors: Design, Synthesis, In silico Studies, and Anti-proliferative Assessment
...Show More Authors
Background:

1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.

Objectives:

To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.

Methods:

The designed compounds were synthesized using conventional organic synthesis methods. The antitumor activities of the new NF derivatives against HepG2 hepatocellular carcinoma and A549 non-small cell lung cancer cell lines were assessed in vitro via MTT assay, flow cytometry, RT-PCR, as well as via molecular docking studies.

Results:

The cytotoxicity results indicated that the newly synthesized NF derivatives were cytotoxic against the two cancer cell lines, with compound 6 being the most cytotoxic, achieving the lowest IC50 concentration. Furthermore, compound 6 targeted EGFR tyrosine kinase leading to cell cycle arrest at the G2/M cell cycle phase and induction of apoptosis. The in vitro biological investigation results matched those of the molecular docking analysis. In conclusion, the new NF derivatives, specifically compound 6, exhibited favorable pharmacokinetic features and are promising EGFR tyrosine kinase inhibitors.

Conclusion:

A series of niflumic acid derivatives (3, 4A-E, 5, and 6) were successfully created, and FT-IR, 1H, 13CNMR, and HRMS were used to confirm their chemical structures. According to molecular docking studies, compounds 3, 5, and 6 have the highest docking scores (ΔG), and most tested compounds have a good pharmacokinetic profile. Results of compound 6 in vitro antitumor activities showed that it is a promising EGFR tyrosine kinase inhibitor.

Scopus Clarivate Crossref
View Publication
Publication Date
Sat Jun 30 2007
Journal Name
Al-kindy College Medical Journal
Trace Elements in Serum and Seminal Plasma and Their Relationship to Infertility in Iraqi Males
...Show More Authors

Background: Environmental chemicals are thought to
adversely affect human reproductive function.
Objective : To estimate the concentration of cadmium(Cd)
, lead ( Pb ) and Zinc ( Zn ) in serum and seminal plasma
among infertile men .
Methods: A sample of 70 infertile men was investigated.
The relationship of trace elements concentration in serum and
seminal plasma was studied in relation to sperm density,
motility and sperm count.
Results: Except for Zinc the concentration of (Pb) and (Cd)
were generally higher in serum than in seminal plasma. The
mean concentration of (Zn) in seminal plasma was more than
25 times higher than in serum There were no statistical
significant differences observed in the

... Show More
View Publication Preview PDF
Publication Date
Mon Mar 07 2022
Journal Name
Book
Insights into developing curricula in mass communication departments and colleges in public and private universities
...Show More Authors

Technology developed at very rapid paces in the last decade of the twentieth century and what followed, especially communication technology, as the World Wide Web appeared in the mid-nineties of the last century, Facebook in 2004 and 2006, the mobile phone, 1993, 1994, and social networking sites. The other. These technological developments have had an impact on societies, whether among individuals in one country or among different peoples. The citizen in any part of the world has become a journalist who practices the work of a specialized or professional journalist, even if he does not know how to read and write, or has a low level of education, as he can now transmit events from wherever he is to the world, through his personal page, or v

... Show More
Preview PDF
Publication Date
Tue Mar 30 2021
Journal Name
College Of Islamic Sciences
Need and transgression in Surat (Abs) Semantic grammatical study: Need and transgression in Surat (Abs)
...Show More Authors

      The research aims to highlight the significance and composition and the diversity of meanings and the Quranic context in the necessary and transgressive verbs in Surat (Abs).

      This research consists of : a preamble , and two studies . The researcher addressed in the preliminary the importance of the phenomenon of necessity and infringement, the signs of the necessary action , the structure and controls of the act , the methods of infringement , its sections and signs.

      As for the first topic : The researcher addressed the necessary verbs in Surat Abs , an applied study in terms of grammati

... Show More
View Publication Preview PDF
Publication Date
Sat Feb 09 2019
Journal Name
Journal Of The College Of Education For Women
Employment and Societal Changes in Iraq Challenges and Policies
...Show More Authors

This study attempts to focus on there lation ship between employment policies andsocietal changesinIraq.Theconstruction ofoperational policyincommunitiesin crisis remains fraught with challenges and risks, especially in countries that have longoutstanding conflict sand crises, it is important in this context to achieve those policy and build the foundations of human security and poverty alleviation, unemployment, to find effective ways to help the community to achieve stability and reduce the risk of renew edorrepeat the cycleofviolence-butthatwouldrequirearadicalrethinking, including rethinking the way evaluating therisksandchallengesand management.And thatsuchaprojectshouldbe based ona clear roadmap, andthevisionsofdevelopmentanda clea

... Show More
View Publication Preview PDF
Publication Date
Thu Jun 30 2016
Journal Name
Al-kindy College Medical Journal
Obesity and its co morbidities in children and adolescents
...Show More Authors

Background: Obesity has become one of the most important public heath problems all over the world.An epidemic of obesity is affecting children and adolescents across the developed and developing countries in recent years. As the prevalence of obesity increased, so did the prevalence of co morbidities like metabolic and endocrine diseases.Objectives: To overview obesity clinical features and the prevalence of associated co morbidities in children and adolescents attended the obesity researches and therapy center in Alkindy medical collage.Type of study: This is a cohort observational studyMethods : Obese child and adolescents aged 4-15year attended the obesity research and therapy unit in AL Kindy medical collage from the 1st of September

... Show More
View Publication Preview PDF
Publication Date
Wed Dec 07 2011
Journal Name
Journal Of Planner And Development
centralization and decentralization in Iraq and its future prospects
...Show More Authors

Centralization and decentralization, planning and development, and community participation in the management of its affairs and to activate all the abilities that multiple methods aimed at creating the proper environment for the growth and development of society in the place where he lives. As long as the overall trend in Iraq, represented by the Permanent Constitution of decentralization to regions and provinces, the solutions to the obstacles that may face this transition in some respects presents ways of coordination and integration between multiple levels of planning which can be exercised by the schematic in the future the organization. In this paper some of the visions and ideas that can  contribute to the organization

... Show More
View Publication Preview PDF
Publication Date
Sat Aug 01 2015
Journal Name
Journal Of Engineering
Values and technology in architecture - the impact and vulnerability
...Show More Authors

Technology is an important factor for achieving architecture as an impact and vulnerability. It represents one of the significant elements in creating the intellectual framework, as well as having its own intellectual breakdown, while values constitute the most important and obviously factor of the community's intellectual. Research aims was determined accordingly by: investigating the role and impact of values and their relationship to technology in architecture.

In this context, the research investigated values and technology in architecture, through discussing their aspects and dimensions in architecture. In the context of values, the research discussed their concept and the related ones to have a concrete def

... Show More
View Publication Preview PDF
Publication Date
Sun Jun 02 2019
Journal Name
Journal Of The College Of Languages (jcl)
The Exploitation of Carmen Valero Garces' Theory in the Criticism of Literary Texts: Saleh al-Jafari's Arabic Translation of "Rubbayat al-Khayyam" as a: کاربست نظریه¬ی کارمن والرو گارسس در نقد ترجمه¬ی ادبی (مورد مطالعه: تعریب صالح الجعفری از رباعیات خیام)
...Show More Authors

There is a mutual relationship between the form of a text and its meaning so as separating these two or devaluating the role of one of them leads to the absence of the value therein. Thus, a translation is important as to how it relates the details of a text. That is, the text has special features which go beyond form, and these set out its distinctiveness. Here, we tackle Saleh al-Jafari's Arabic translation of  "Rubbayat al-Khayyam" of Naysapour descriptively and analytically by depending on extracts from the original text. This translation is evaluated on the basis of Spanish critic Maria Carmen Valero Garces. Herein, we discuss the effectiveness of this theory in the criticism of literary texts. It has been concluded that al-Jaf

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Jan 22 2020
Journal Name
Molecules
In Vivo and In Vitro Evaluation of the Protective Effects of Hesperidin in Lipopolysaccharide-Induced Inflammation and Cytotoxicity of Cell
...Show More Authors

(1) Background: Plant flavonoids are efficient in preventing and treating various diseases. This study aimed to evaluate the ability of hesperidin, a flavonoid found in citrus fruits, in inhibiting lipopolysaccharide (LPS) induced inflammation, which induced lethal toxicity in vivo, and to evaluate its importance as an antitumor agent in breast cancer. The in vivo experiments revealed the protective effects of hesperidin against the negative LPS effects on the liver and spleen of male mice. (2) Methods: In the liver, the antioxidant activity was measured by estimating the concentration of glutathione (GSH) and catalase (CAT), whereas in spleen, the concentration of cytokines including IL-33 and TNF-α was measured. The in vitro expe

... Show More
View Publication
Scopus (40)
Crossref (34)
Scopus Clarivate Crossref
Publication Date
Mon Jan 01 2018
Journal Name
International Journal Of Chemtech Research
Liquid Chromatographic and validation study in separation and determination of benzidines and phenols in the main discharge point of wastewater
...Show More Authors

View Publication
Crossref