Preferred Language
Articles
/
mRd8LZIBVTCNdQwC3KcL
Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
...Show More Authors
Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR, and HR-mass spectroscopy.

Results:

Compound S4 had a relatively high pharmacophore-fit score, indicating that it may have biological activity similar to the EGFR allosteric inhibitor reference, and it scored a relatively low ΔG against EGFR TK allosteric site, indicating a high likelihood of drug-receptor complex formation. Compound S4 was cytotoxic to the three cancer cell lines tested, particularly HCT-116 colorectal cancer cells, with an IC50 value comparable to Erlotinib. Compound S4 induced the intrinsic apoptotic pathway in HCT-116 cells by arresting them in the G2/M phase. All of the new derivatives, including S4, met the in silico requirements for EGFR allosteric inhibitory activity.

Conclusion:

Compound S4 is a promising EGFR tyrosine kinase allosteric inhibitor that warrants further research.

Scopus Clarivate Crossref
View Publication
Publication Date
Tue Dec 01 2020
Journal Name
Systematic Reviews In Pharmacy)srp)
Evaluation the response to infliximab therapy in patients with ulcerative colitis and crohn's disease
...Show More Authors

Scopus (1)
Scopus
Publication Date
Wed Dec 01 2010
Journal Name
Al Mustansiriyah Journal Of Pharmaceutical Sciences
Evaluation ofAaspirin, Clopidogrel or Their Combination In Hypertensive Patients
...Show More Authors

The objective of this study is to evaluate the effect of aspirin, clopidogrel or their combination on different parameters in hypertensive patients.Platelets adhesion, activation, and aggregation are central to thrombus formation, which follows atherosclerotic plaque disruption and causes acute coronary syndromes. Aspirin and clopidogrel exert their antiplatelet effects by inhibiting thromboxane A2 production and adenosine diphosphate–induced platelet aggregation pathways, respectively. This study was designed to evaluate the possible effects of aspirin and clopidogrel given either alone or in combination in patients with essential hypertension on blood pressure and other parameters in addition to lipid profile using a randomized

... Show More
Crossref
Publication Date
Tue Feb 05 2019
Journal Name
Journal Of The College Of Education For Women
Effectiveness of Woman's Personality between the Public and Private Event the Novel Feminist Iraqi 2003 - 2013
...Show More Authors

After we completed this book search we must extraction most important the findings.
Event of war a majar impact on same as all human being but signed and its impact in the
psyche of iraqi woman unparalleled result of the suffering that were produced by these wars
that contributed to the destabilization of Her life at all levels a woman has lost her father,
husband and son an brother as well as extreme poverty caused by the economic blockade
brought in to existence wars that exacerbated the suffering was the woman to work and
economic in order to provide a living for her and her family and pre – empt the dreams and
ambitions so he excelled writer Iraqi in portraying the succession of wars that ate every thing
and

... Show More
View Publication Preview PDF
Publication Date
Thu Jan 04 2018
Journal Name
International Journal Of Molecular Sciences
Understanding the Progression of Bone Metastases to Identify Novel Therapeutic Targets
...Show More Authors

View Publication
Scopus (40)
Crossref (31)
Scopus Clarivate Crossref
Publication Date
Fri Dec 07 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Novel Combination for Self-Nanoemulsifying Drug Delivery System of Candesartan Cilexetil
...Show More Authors

Solubility problem of many of effective pharmaceutical molecules are still one of the major obstacle in theformulation of such molecules. Candesartan cilexetil (CC) is angiotensin II receptor antagonist with very low water solubility and this result in low and variable bioavailability. Self- emulsifying drug delivery system (SEDDS) showed promising result in overcoming solubility problem of many drug molecules. CC was prepared as SEDDS by using novel combination of two surfactants (tween 80 and cremophore EL) and tetraglycol as cosurfactant, in addition to the use of triacetin as oil. Different tests were performed in order to confirm the stability of the final product which includes thermodynamic study, determination of self-emulsificat

... Show More
View Publication Preview PDF
Scopus (7)
Crossref (1)
Scopus Crossref
Publication Date
Wed May 08 2024
Journal Name
Babylon: Abjad Publising House
“Translation is the Art of Negotiating with Words”, in Hassad aS-Sineen(Harvest of Years): Essays in Teaching Translation
...Show More Authors

Publication Date
Mon Mar 15 2021
Journal Name
Al-academy
Anthropology and Representations of Magic in Arab Theatrical Text Harut and Marut's Play as a Model: وصال خلفة كاظم البكري
...Show More Authors

The research (Anthropology and Representations of magic in Arab Theatrical Text, Harut and Marut's play as a Model) is concerned with studying magic and the forms of its presence in the theatrical text in different human cultures where it belongs. The research consists of four chapters.
The first chapter includes the research problem that revolves around the following questions: (what is the mechanism of employing magic anthropology and its representations in the Arab theatrical text Harut and Marut's play as a model?), and the research importance which is attributed to the necessity of studying (magic) in the Arab theatrical text as it is considered the inauguration of one of the social phenomena that many researchers in the field o

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sat Sep 01 2018
Journal Name
Iraqi Journal Of Science
Estimate Antimicrobial activity and Anti-biofilm formation of bark Cinnamomum zeylanicum on Klebsiella pneumoniae isolated from Urinary Tract Infections
...Show More Authors

View Publication
Scopus (5)
Crossref (1)
Scopus Crossref
Publication Date
Tue Jun 02 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, characterization and Study Bioactivity of Silver Nanocomposites
...Show More Authors

View Publication Preview PDF
Scopus (1)
Scopus Crossref
Publication Date
Sun Sep 06 2015
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Antibacterial Activity of Cefalexin Dervatives
...Show More Authors

New series of Schiff bases 2(a-j) and corresponding beta-lactam derivatives 3(a-j) were synthesized from cefalexin (1) as starting material. The compound (1) was reacted with different aldehydes and ketones to give Schiff bases derivatives 2(a-j). The synthesized Schiff bases were cyclized by chloroacetyl chloride in the presence of triethylamine to form beta-lactam derivatives 3(a-j). The compounds were characterized by deremination melting point, FT-IR and 1H NMR. The beta-lactam derivatives were screened in vitro antibacterial against some bacterial species

View Publication Preview PDF
Crossref (1)
Crossref