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
Sat May 23 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of the cleaning efficiency of the isthmus using different rotary instrumentation techniques (In vitro study)
...Show More Authors

Background: The aims of the study were to evaluate the unclean/clean root canal surface areas with a histopathological cross section view of the root canal and the isthmus and to evaluate the efficiency of instrumentation to the isthmus using different rotary instrumentation techniques. Materials and Methods:The mesial roots of thirty human mandibular molars were divided into six groups, each group was composed of five roots (10 root canals)which prepared and irrigated as: Group one A: Protaper system to size F2 and hypodermic syringe, Group one B: Protaper system to size F2 and endoactivator system, Group two A:Wave One small then primary file and hypodermic syringe, Group two B:Wave One small then primary file and endoactivator system, Gr

... Show More
View Publication Preview PDF
Publication Date
Tue Jan 20 2026
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization and Dyeing Performance of Co(II), Ni(II), Cu(II) and Zn(II) Complexes with (E)-4-Chloro-N-(2-(Dimethylamino)Ethyl)-5-((8-Hydroxyquinolin-5-yl)Diazenyl)-2-Methoxybenzamide
...Show More Authors

The (E)-4-chloro-N-(2-(dimethylamino)ethyl)-5-((8-hydroxy quinolin-5-yl)diazenyl)-2-methoxybenzamide azo ligand (L) has been synthesized through the reaction of diazonium salt for 5-amino-4-chloro-N-(2-(dimethylamino) ethyl)-2-methoxybenzamide with 8-hydroxyquinoline and identified azo ligand (L) using spectroscopic studies (FTIR, UV-Vis, 1H and 13CNMR, mass), and micro-elemental analysis (C.H.N). Metal chelates of Co(II), Ni(II), Cu(II), as well as Zn(II) have been completed as well as characterized using mass spectra, flame atomic absorption, elemental analysis (C.H.N), infrared, UV-Vis spectroscopy, as well as conductivity, magnetic measurements. The metal-to-ligand ratio in all complexes, as determined by analytical data, was 1:2 and ex

... Show More
Publication Date
Sat Aug 01 2020
Journal Name
Nanotechnology For Environmental Engineering
Synthesis of Ni@γ-Al2O3@PID\SiW recyclable nanocatalyst and its catalytic reduction and antibacterial activities
...Show More Authors

Scopus (11)
Crossref (8)
Scopus Crossref
Publication Date
Thu Dec 01 2022
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis, Identification and Study of Antioxidant and Anticancer Activities of New 2-Substituted-1,3,4-Thiadiazole from Creatinine
...Show More Authors

View Publication
Scopus (4)
Crossref (2)
Scopus Clarivate Crossref
Publication Date
Sun Jun 30 2013
Journal Name
Al-kindy College Medical Journal
Cognitive Effects of Tumor and Surgical Treatment in Patients with Cerebral Gliomas
...Show More Authors

Background: Quality of life in brain tumor patients is an emerging issue and has prompted neurosurgeons to recon¬sider the need for cognitive assessment in the course of treatment. To date there has been a lack of comprehensive neuropsychological assessment performed preoperatively and in the acute postoperative period in our hospitals.Objectives: to establish the effects of tumors and their surgical treatment, from a neuropsychological perspective, on cognitive functioning in patients with cerebral Gliomas. Methods: This is a prospective study conducted in the Neurosurgical Hospital in Baghdad, Iraq, during the period from January 1999 to January 2001. Any patient admitted during the period of the study with clinical history, signs, sy

... Show More
View Publication Preview PDF
Publication Date
Tue May 29 2018
Journal Name
Journal Of Pharmaceutical And Scientific Research
Synthesis and characterization of substituted 1, 2,4-triazole and their derivatives on poly ethylene
...Show More Authors

Abstract New derivatives of 1,2,4- triazole , 1,2,4-triazole -3-one and 1,2,4-triazole-3-thione were obtained through this research. Acid hydrazide derivative was present from reaction of poly acryloyl chloride with hydrazine hydrate in presence of DMF as a solvent then reacted with benzonitrile and its derivatives to give 1,2,4-triazole derivatives. After that reaction of poly acryloyl chloride with semicarbazide and semithiocarbazide to form semicarbazone and semithiocarbazone derivatives respectively. Finally, closing of semicarbazone and semithiocarbazone derivatives with 2% NaOH gave 1,2,4-triazole -3-one and 1,2,4-triazole-4-thione derivatives respectively. These new synthesized products have been characterized by infrared, 1 H-n

... Show More
Publication Date
Sun Mar 03 2013
Journal Name
Journal Of Al-nahrain University
Synthesis and Characterization of Some New 1,2,3-Triazole, Pyrazolin-5-one and thiazolidinone Derivatives
...Show More Authors

Five membered heterocyclics derivatives were synthesized in this work by three routes. The first route includes the synthesis of N-benzoic acid 1,2,3,-triazole derivatives (3),(4) by diazotation of methyl-2-amino benzoate and treating the resulted salt (1) with sodium azide and ethyl acetoacetate or acetyl acetone, respectively. In the second route, derivatives of pyrazole (8) pyrazolin-5-one (9), (10) were prepared by the reaction of the salt (1) with some active methylene compounds to give the corresponding hydrazones derivatives (5-7) which then they were treated with hydrazine hydrate. The third route afforded the synthesis of three derivatives (12), (15a), (15b) of thiazolidinone by two different methods. AII compounds were confirmed b

... Show More
Preview PDF
Publication Date
Mon Mar 01 2010
Journal Name
Journal Of Kerbala University
Synthesis And Biological Activity Of Some New Compounds Containing 1,2,4-Triazole And Their Derivatives
...Show More Authors

Condensation of 1,2- dibromo ethane with para hydroxy benzoic acid gave 1,2-Ethane-bis- 4-oxybenzoic [1]. This Compound was converted with the thionyl chloride to give 1,2-Ethane-bis- 4-oxybenzoyl chloride [2]. Reaction of compound [2] with thiosemicarbizades gave 1,2-Ethanebis[4-oxybenzoyl-thiosemicarbazide] [3] and opteined 1,2-Ethane-bis[3-mercapto-5-phenoxy- 1,2,4-triazole] [4] from treatment compound [3] with NaOH (4%) .The new compounds 1,2- Ethane-bis[3-(substituted thioacyl)-4-(substituted acyl)-5 phenoxy-1,2,4-triazole] [5a-d] and 1,2- Ethane-bis[3-(substituted alkylthio)-5 phenoxy-1,2,4-trizole] [5e-f] derived from compound [4] were synthesized and characterized by physical and spectral data. All the compounds [4], [5a-d] and [5e-

... Show More
Publication Date
Sat Jan 06 2018
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis and characterization of substituted 1, 2,4-triazole and their derivatives on poly ethylene
...Show More Authors

Scopus (13)
Scopus
Publication Date
Fri Dec 01 2023
Journal Name
Food Bioscience
Green synthesis of silver nanomaterials and evaluation of their antibacterial and antioxidant effectiveness in chicken meat
...Show More Authors

View Publication
Scopus (10)
Crossref (8)
Scopus Clarivate Crossref