A review on progression of epidermal growth factor receptor (EGFR) inhibitors as an efficient approach in cancer targeted therapy

A Ayati, S Moghimi, S Salarinejad, M Safavi… - Bioorganic …, 2020 - Elsevier
The identification of molecular agents inhibiting specific functions in cancer cells
progression is considered as one of the most successful plans in cancer treatment. The …

Advances in covalent kinase inhibitors

A Abdeldayem, YS Raouf, SN Constantinescu… - Chemical Society …, 2020 - pubs.rsc.org
Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

Pyrimidine-based EGFR TK inhibitors in targeted cancer therapy

A Ayati, S Moghimi, M Toolabi, A Foroumadi - European Journal of …, 2021 - Elsevier
Despite significant improvements of new treatment options, cancer continues to represent as
one of the most common and fatal disease. The EGFR signaling pathway is considered as a …

An outlook of docking analysis and structure-activity relationship of pyrimidine-based analogues as EGFR inhibitors against non-small cell lung cancer (NSCLC)

R Pal, G Teli, S Sengupta, L Maji… - Journal of …, 2024 - Taylor & Francis
Almost 80% of lung cancer diagnoses each year correspond to non-small cell lung cancer
(NSCLC). The percentage of NSCLC with EGFR overexpression ranges from 40% to 89 …

Design, synthesis, antiproliferative evaluation, and molecular docking study of new quinoxaline derivatives as apoptotic inducers and EGFR inhibitors

EA Fayed, YA Ammar, MA Saleh, AH Bayoumi… - Journal of Molecular …, 2021 - Elsevier
A new series of quinoxaline derivatives synthesized and pharmacologically evaluated
against (HepG-2, HCT-116, and MCF-7) cell lines. Seven compounds were found to …

Development of adamantane scaffold containing 1, 3, 4-thiadiazole derivatives: Design, synthesis, anti-proliferative activity and molecular docking study targeting …

MMS Wassel, YA Ammar, GAME Ali, A Belal… - Bioorganic …, 2021 - Elsevier
Abstract A new series of 1, 3, 4-thiadiazolo-adamantane derivatives were synthesized
through molecular hybridization approach, then used as starting material to synthesize …

Epidermal growth factor receptor inhibitors as potential anticancer agents: An update of recent progress

B Sharma, VJ Singh, PA Chawla - Bioorganic Chemistry, 2021 - Elsevier
Epidermal growth factor receptor (EGFR) is a vital intermediate in cell signaling pathway
including cell proliferation, angiogenesis, apoptosis, and metastatic spread and also having …

Discovery of dosimertinib, a highly potent, selective, and orally efficacious deuterated EGFR targeting clinical candidate for the treatment of non-small-cell lung cancer

Y Meng, B Yu, H Huang, Y Peng, E Li… - Journal of medicinal …, 2021 - ACS Publications
Osimertinib is a highly potent and selective third-generation epidermal growth factor
receptor (EGFR) inhibitor, which provides excellent clinical benefits and is now a standard-of …

An assessment of EGFR and HER2 inhibitors with structure activity relationship of fused pyrimidine derivatives for breast cancer: a brief review

PS Dhiwar, GS Purawarga Matada, R Pal… - Journal of …, 2024 - Taylor & Francis
Epidermal growth factor receptor (EGFR) and its subtype human epidermal growth factor
receptor 2 (HER2) gets activated when its endogenous ligand (s) bind to its ATP binding site …

Selective covalent targeting of mutated EGFR (T790M) with chlorofluoroacetamide-pyrimidines

M Sato, H Fuchida, N Shindo, K Kuwata… - ACS Medicinal …, 2020 - ACS Publications
Covalent modification of disease-associated proteins with small molecules is a powerful
approach for achieving an increased and sustained pharmacological effect. To reduce the …