Cargando…

Novel 2-(5-Aryl-4,5-Dihydropyrazol-1-yl)thiazol-4-One as EGFR Inhibitors: Synthesis, Biological Assessment and Molecular Docking Insights

INTRODUCTION: Epidermal growth factor receptor (EGFR) regulates several cell functions which include cell growth, survival, multiplication, differentiation, and apoptosis. Currently, EGFR kinase inhibitors are of increasing interest as promising targeted antitumor therapeutic agents. METHODS: Differ...

Descripción completa

Detalles Bibliográficos
Autores principales:	Al-Warhi, Tarfah, El Kerdawy, Ahmed M, Said, Mohamed A, Albohy, Amgad, Elsayed, Zainab M, Aljaeed, Nada, Elkaeed, Eslam B, Eldehna, Wagdy M, Abdel-Aziz, Hatem A, Abdelmoaz, Miral A
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Dove 2022
Materias:	Original Research
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9123247/ https://www.ncbi.nlm.nih.gov/pubmed/35607598 http://dx.doi.org/10.2147/DDDT.S356988

Ejemplares similares

Design, synthesis, in vitro biological assessment and molecular modeling insights for novel 3-(naphthalen-1-yl)-4,5-dihydropyrazoles as anticancer agents with potential EGFR inhibitory activity
por: Eldehna, Wagdy M., et al.
Publicado: (2022)

Identification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights
por: Eldehna, Wagdy M., et al.
Publicado: (2022)

Synthesis, Biological Evaluation and In Silico Studies of Certain Oxindole–Indole Conjugates as Anticancer CDK Inhibitors
por: Al-Warhi, Tarfah, et al.
Publicado: (2020)

Novel oxindole/benzofuran hybrids as potential dual CDK2/GSK-3β inhibitors targeting breast cancer: design, synthesis, biological evaluation, and in silico studies
por: Eldehna, Wagdy M., et al.
Publicado: (2020)

Discovery of 2,4-thiazolidinedione-tethered coumarins as novel selective inhibitors for carbonic anhydrase IX and XII isoforms
por: Eldehna, Wagdy M., et al.
Publicado: (2022)

Design and synthesis of benzothiazole-based SLC-0111 analogues as new inhibitors for the cancer-associated carbonic anhydrase isoforms IX and XII
por: Al-Warhi, Tarfah, et al.
Publicado: (2022)

Development of novel isatin–nicotinohydrazide hybrids with potent activity against susceptible/resistant Mycobacterium tuberculosis and bronchitis causing–bacteria
por: Elsayed, Zainab M., et al.
Publicado: (2021)

1-Benzyl-5-bromo-3-hydrazonoindolin-2-ones as Novel Anticancer Agents: Synthesis, Biological Evaluation and Molecular Modeling Insights
por: Al-Warhi, Tarfah, et al.
Publicado: (2023)

Discovery of 3,6-disubstituted pyridazines as a novel class of anticancer agents targeting cyclin-dependent kinase 2: synthesis, biological evaluation and in silico insights
por: Sabt, Ahmed, et al.
Publicado: (2020)

Identification of Novel Cyanopyridones and Pyrido[2,3-d]pyrimidines as Anticancer Agents with Dual VEGFR-2/HER-2 Inhibitory Action: Synthesis, Biological Evaluation and Molecular Docking Studies
por: Al-Warhi, Tarfah, et al.
Publicado: (2022)

Formation of 1-(thiazol-2-yl)-4,5-dihydropyrazoles from simple precursors: synthesis, spectroscopic characterization and the structures of an intermediate and two products
por: Mahesha, Ninganayaka, et al.
Publicado: (2021)

Identification of a New Potential SARS-COV-2 RNA-Dependent RNA Polymerase Inhibitor via Combining Fragment-Based Drug Design, Docking, Molecular Dynamics, and MM-PBSA Calculations
por: El Hassab, Mahmoud A., et al.
Publicado: (2020)

1-[5-(3,4-Dichlorophenyl)-3-(2-naphthyl)-4,5-dihydropyrazol-1-yl]ethanone
por: Lu, Zhi-Ke, et al.
Publicado: (2008)

Synthesis, biological evaluation and molecular docking of new triphenylamine-linked pyridine, thiazole and pyrazole analogues as anticancer agents
por: Elmorsy, Mohamed R., et al.
Publicado: (2022)

Synthesis and in vitro anticancer activity of certain novel 1-(2-methyl-6-arylpyridin-3-yl)-3-phenylureas as apoptosis-inducing agents
por: Eldehna, Wagdy M., et al.
Publicado: (2019)

2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights
por: Elbadawi, Mostafa M., et al.
Publicado: (2021)

Synthesis, in silico studies and biological screening of (E)-2-(3-(substitutedstyryl)-5-(substitutedphenyl)-4,5-dihydropyrazol-1-yl)benzo[d]thiazole derivatives as an anti-oxidant, anti-inflammatory and antimicrobial agents
por: Kumar, Manoj, et al.
Publicado: (2022)

Conversion of diarylchalcones into 4,5-dihydropyrazole-1-carbothioamides: molecular and supramolecular structures of two precursors and three products
por: Shaibah, Mohammed A. E., et al.
Publicado: (2020)

Development of Novel Isatin-Tethered Quinolines as Anti-Tubercular Agents against Multi and Extensively Drug-Resistant Mycobacterium tuberculosis
por: Abdelrahman, Mohamed A., et al.
Publicado: (2022)

GC-MS metabolites profiling of anethole-rich oils by different extraction techniques: antioxidant, cytotoxicity and in-silico enzymes inhibitory insights
por: El-Kersh, Dina M., et al.
Publicado: (2022)

Chemical composition, seasonal variation and antiaging activities of essential oil from Callistemon subulatus leaves growing in Egypt
por: Rabie, Omyma, et al.
Publicado: (2023)

Synthesis of 2-(4,6-Dimethoxy-1,3,5-triazin-2-yloxyimino) Derivatives: Application in Solution Peptide Synthesis
por: Al-Warhi, Tarfah I., et al.
Publicado: (2010)

Enaminone-based carboxylic acids as novel non-classical carbonic anhydrases inhibitors: design, synthesis and in vitro biological assessment
por: Abo-Ashour, Mahmoud F., et al.
Publicado: (2022)

Olive Leaves as a Potential Phytotherapy in the Treatment of COVID-19 Disease; A Mini-Review
por: Abdelgawad, Shimaa M., et al.
Publicado: (2022)

Design, synthesis and antibacterial potential of 5-(benzo[d][1,3]dioxol-5-yl)-3-tert-butyl-1-substituted-4,5-dihydropyrazoles
por: El-Behairy, Mohammed F., et al.
Publicado: (2015)

Development of novel isatin thiazolyl-pyrazoline hybrids as promising antimicrobials in MDR pathogens
por: Al-Warhi, Tarfah, et al.
Publicado: (2022)

Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules
por: Elkaeed, Eslam B., et al.
Publicado: (2021)

Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer
por: Eldehna, Wagdy M., et al.
Publicado: (2021)

Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity
por: Kassab, Refaie M, et al.
Publicado: (2022)

New [1,2,4]triazolo[4,3-c]quinazolines as intercalative Topo II inhibitors: Design, synthesis, biological evaluation, and in silico studies
por: Gaber, Ahmed A., et al.
Publicado: (2023)

Identification of new 4-(6-oxopyridazin-1-yl)benzenesulfonamides as multi-target anti-inflammatory agents targeting carbonic anhydrase, COX-2 and 5-LOX enzymes: synthesis, biological evaluations and modelling insights
por: Badawi, Waleed A., et al.
Publicado: (2023)

Novel [(N-alkyl-3-indolylmethylene)hydrazono]oxindoles arrest cell cycle and induce cell apoptosis by inhibiting CDK2 and Bcl-2: synthesis, biological evaluation and in silico studies
por: Al-Warhi, Tarfah, et al.
Publicado: (2020)

Development of 2-oindolin-3-ylidene-indole-3-carbohydrazide derivatives as novel apoptotic and anti-proliferative agents towards colorectal cancer cells
por: Eldehna, Wagdy M., et al.
Publicado: (2020)

Design and synthesis of thiazolidine-2,4-diones hybrids with 1,2-dihydroquinolones and 2-oxindoles as potential VEGFR-2 inhibitors: in-vitro anticancer evaluation and in-silico studies
por: Taghour, Mohammed S., et al.
Publicado: (2022)

Design and Synthesis of New 2-Aryl-4,5-dihydro-thiazole Analogues: In Vitro Antibacterial Activities and Preliminary Mechanism of Action
por: Tan, Fangfang, et al.
Publicado: (2015)

Biological evaluation, docking studies, and in silico ADME prediction of some pyrimidine and pyridine derivatives as potential EGFR(WT) and EGFR(T790M) inhibitors
por: Al-Warhi, Tarfah, et al.
Publicado: (2022)

Synthesis and Biological Screening of New 2-(5-Aryl-1-phenyl-1H-pyrazol-3-yl)-4-aryl Thiazole Derivatives as Potential Antimicrobial Agents
por: Nandurkar, Yogesh, et al.
Publicado: (2023)

Direct N-heterocyclization of hydrazines to access styrylated pyrazoles: synthesis of 1,3,5-trisubstituted pyrazoles and dihydropyrazoles
por: Venkateswarlu, Vunnam, et al.
Publicado: (2018)

Design and synthesis of novel rigid dibenzo[b,f]azepines through ring closure technique as promising anticancer candidates against leukaemia and acting as selective topoisomerase II inhibitors and DNA intercalators
por: El-Behairy, Mohammed Farrag, et al.
Publicado: (2023)

Design, synthesis, anti-proliferative evaluation, docking, and MD simulations studies of new thiazolidine-2,4-diones targeting VEGFR-2 and apoptosis pathway
por: Taghour, Mohammed S., et al.
Publicado: (2022)

Cannot write session to /tmp/vufind_sessions/sess_vaahi83v67sm83vjantorgn8mk