Cargando…

Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFR(WT) and EGFR(T790M)

New 1H-pyrazolo[3,4-d]pyrimidine derivatives were designed and synthesised to act as epidermal growth factor receptor inhibitors (EGFRIs). The synthesised derivatives were assessed for their in vitro anti-proliferative activities against A549 and HCT-116 cancer cells. Compounds 8, 10, 12a, and 12b s...

Descripción completa

Detalles Bibliográficos
Autores principales:	Gaber, Ahmed A., Sobhy, Mohamed, Turky, Abdallah, Abdulwahab, Hanan Gaber, Al-Karmalawy, Ahmed A., Elhendawy, Mostafa. A., Radwan, Mohamed. M., Elkaeed, Eslam B., Ibrahim, Ibrahim M., Elzahabi, Heba S. A., Eissa, Ibrahim H.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Taylor & Francis 2022
Materias:	Research Paper
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9466626/ https://www.ncbi.nlm.nih.gov/pubmed/36000168 http://dx.doi.org/10.1080/14756366.2022.2112575

Ejemplares similares

New Anticancer Theobromine Derivative Targeting EGFR(WT) and EGFR(T790M): Design, Semi-Synthesis, In Silico, and In Vitro Anticancer Studies
por: Elkaeed, Eslam B., et al.
Publicado: (2022)

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)

Design, synthesis, and anti-cancer evaluation of new pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis inducers
por: Elzahabi, Heba S. A., et al.
Publicado: (2022)

Design, synthesis, docking, MD simulations, and anti-proliferative evaluation of thieno[2,3-d]pyrimidine derivatives as new EGFR inhibitors
por: Sobh, Eman A., et al.
Publicado: (2023)

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)

Recruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFR(WT), EGFR(T790M), and EGFR(L858R))
por: Abo Al-Hamd, Mahmoud G., et al.
Publicado: (2023)

Anticancer derivative of the natural alkaloid, theobromine, inhibiting EGFR protein: Computer-aided drug discovery approach
por: Eissa, Ibrahim H., et al.
Publicado: (2023)

Synthesis, biological evaluation, and in silico studies of new CDK2 inhibitors based on pyrazolo[3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffold with apoptotic activity
por: Mandour, Asmaa A., et al.
Publicado: (2022)

Discovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation
por: Hagras, Mohamed, et al.
Publicado: (2021)

A New Anticancer Semisynthetic Theobromine Derivative Targeting EGFR Protein: CADDD Study
por: Eissa, Ibrahim H., et al.
Publicado: (2023)

Computer-Assisted Drug Discovery of a Novel Theobromine Derivative as an EGFR Protein-Targeted Apoptosis Inducer
por: Eissa, Ibrahim H, et al.
Publicado: (2023)

Thieno[2,3-b]thiophene Derivatives as Potential EGFR(WT) and EGFRT(790M) Inhibitors with Antioxidant Activities: Microwave-Assisted Synthesis and Quantitative In Vitro and In Silico Studies
por: Ahmed, Sanaa A., et al.
Publicado: (2022)

Topo II inhibition and DNA intercalation by new phthalazine-based derivatives as potent anticancer agents: design, synthesis, anti-proliferative, docking, and in vivo studies
por: Khalifa, Mohamed M., et al.
Publicado: (2021)

Design, synthesis, anti-proliferative evaluation, docking, and MD simulation studies of new thieno[2,3-d]pyrimidines targeting VEGFR-2
por: El-Metwally, Souad A., et al.
Publicado: (2023)

Design, synthesis, and molecular docking studies of novel pomalidomide-based PROTACs as potential anti-cancer agents targeting EGFR(WT) and EGFR(T790M)
por: O. Aboelez, Moustafa, et al.
Publicado: (2022)

Design, synthesis, and biological evaluation of new pyrimidine-5-carbonitrile derivatives as novel anti-cancer, dual EGFR(WT)/COX-2 inhibitors with docking studies
por: Reda, Nada, et al.
Publicado: (2023)

Molecular Docking and Dynamics Simulation Revealed the Potential Inhibitory Activity of ACEIs Against SARS-CoV-2 Targeting the hACE2 Receptor
por: Al-Karmalawy, Ahmed A., et al.
Publicado: (2021)

Identification of new theobromine-based derivatives as potent VEGFR-2 inhibitors: design, semi-synthesis, biological evaluation, and in silico studies
por: Eissa, Ibrahim H., et al.
Publicado: (2023)

In Silico Screening of Semi-Synthesized Compounds as Potential Inhibitors for SARS-CoV-2 Papain-like Protease: Pharmacophoric Features, Molecular Docking, ADMET, Toxicity and DFT Studies
por: Alesawy, Mohamed S., et al.
Publicado: (2021)

A Theobromine Derivative with Anticancer Properties Targeting VEGFR‐2: Semisynthesis, in silico and in vitro Studies
por: Eissa, Ibrahim H., et al.
Publicado: (2023)

Discovery of pyrazolo[3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives as novel CDK2 inhibitors: synthesis, biological and molecular modeling investigations
por: Nassar, Ibrahim F., et al.
Publicado: (2022)

Novel 4-thiophenyl-pyrazole, pyridine, and pyrimidine derivatives as potential antitumor candidates targeting both EGFR and VEGFR-2; design, synthesis, biological evaluations, and in silico studies
por: Al-Muntaser, Samia M., et al.
Publicado: (2023)

Synthesis of Some Novel Pyrazolo[1,5-a]pyrimidine Derivatives and Their Application as Disperse Dyes
por: Al-Etaibi, Alya M., et al.
Publicado: (2011)

EGFR T790M: revealing the secrets of a gatekeeper
por: Ko, Brian, et al.
Publicado: (2017)

Discovery of Potential SARS-CoV-2 Papain-like Protease Natural Inhibitors Employing a Multi-Phase In Silico Approach
por: Elkaeed, Eslam B., et al.
Publicado: (2022)

The Inhibitory Potential of 2′-dihalo Ribonucleotides against HCV: Molecular Docking, Molecular Simulations, MM-BPSA, and DFT Studies
por: Khalil, Ahmed, et al.
Publicado: (2022)

Characterization of Factors Affecting the Detection Limit of EGFR p.T790M in Circulating Tumor DNA
por: Fahoum, Ibrahim, et al.
Publicado: (2018)

Dual MET–EGFR combinatorial inhibition against T790M-EGFR-mediated erlotinib-resistant lung cancer
por: Tang, Z, et al.
Publicado: (2008)

Biological Evaluation and Molecular Docking with In Silico Physicochemical, Pharmacokinetic and Toxicity Prediction of Pyrazolo[1,5-a]pyrimidines
por: Naglah, Ahmed M., et al.
Publicado: (2020)

In Silico Studies of Some Isoflavonoids as Potential Candidates against COVID-19 Targeting Human ACE2 (hACE2) and Viral Main Protease (M(pro))
por: Alesawy, Mohamed S., et al.
Publicado: (2021)

Design, Synthesis, and Antitumor Evaluation of Novel Pyrazolo[3,4-d]pyrimidine Derivatives
por: Kandeel, Manal M., et al.
Publicado: (2012)

In Silico Exploration of Potential Natural Inhibitors against SARS-Cov-2 nsp10
por: Eissa, Ibrahim H., et al.
Publicado: (2021)

Synthesis and Anticancer Activity of Some New Pyrazolo[3,4-d]pyrimidin-4-one Derivatives
por: Abdellatif, Khaled R. A., et al.
Publicado: (2014)

Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c]pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives
por: Abdel Reheim, Mohamed A. M., et al.
Publicado: (2017)

Correction to: Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c] pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives
por: Abdel Reheim, Mohamed A. M., et al.
Publicado: (2017)

A Systematic Review of the Global Intervention for SARS-CoV-2 Combating: From Drugs Repurposing to Molnupiravir Approval
por: Ashour, Nada A, et al.
Publicado: (2022)

EGFR T790M Mutation as a Possible Target for Immunotherapy; Identification of HLA-A*0201-Restricted T Cell Epitopes Derived from the EGFR T790M Mutation
por: Yamada, Teppei, et al.
Publicado: (2013)

Association of EGFR Exon 19 Deletion and EGFR-TKI Treatment Duration with Frequency of T790M Mutation in EGFR-Mutant Lung Cancer Patients
por: Matsuo, Norikazu, et al.
Publicado: (2016)

Combined therapy with EGFR TKI and gambogic acid for overcoming resistance in EGFR-T790M mutant lung cancer
por: WANG, CHENGDE, et al.
Publicado: (2015)

Mutational monitoring of EGFR T790M in cfDNA for clinical outcome prediction in EGFR-mutant lung adenocarcinoma
por: Su, Kang-Yi, et al.
Publicado: (2018)

Cannot write session to /tmp/vufind_sessions/sess_d0fvb548hfthl2obmi9bej8npj