Emerging strategies to overcome resistance to third-generation EGFR inhibitors

K Shi, G Wang, J Pei, J Zhang, J Wang… - Journal of Hematology & …, 2022 - Springer
Epidermal growth factor receptor (EGFR), the receptor for members of the epidermal growth
factor family, regulates cell proliferation and signal transduction; moreover, EGFR is related …

Revealing quinquennial anticancer journey of morpholine: A SAR based review

F Arshad, MF Khan, W Akhtar, MM Alam… - European journal of …, 2019 - Elsevier
Morpholine, a six-membered heterocycle containing one nitrogen and one oxygen atom, is a
moiety of great significance. It forms an important intermediate in many industrial and …

Development of dual inhibitors targeting epidermal growth factor receptor in cancer therapy

L Tan, J Zhang, Y Wang, X Wang, Y Wang… - Journal of Medicinal …, 2022 - ACS Publications
Epidermal growth factor receptor (EGFR) is of great significance in mediating cell signaling
transduction and tumor behaviors. Currently, third-generation inhibitors of EGFR, especially …

Dual target inhibitors based on EGFR: Promising anticancer agents for the treatment of cancers (2017-)

L Hu, M Fan, S Shi, X Song, F Wang, H He… - European Journal of …, 2022 - Elsevier
The EGFR family play a significant role in cell signal transduction and their overexpression
is implicated in the pathogenesis of numerous human solid cancers. Inhibition of the EGFR …

Structure–activity relationship studies based on quinazoline derivatives as EGFR kinase inhibitors (2017–present)

A Șandor, I Ionuț, G Marc, I Oniga, D Eniu, O Oniga - Pharmaceuticals, 2023 - mdpi.com
The epidermal growth factor receptor (EGFR) plays a critical role in the tumorigenesis of
various forms of cancer. Targeting the mutant forms of EGFR has been identified as an …

Design, Synthesis, and Biological Evaluation of Dual Inhibitors of EGFRL858R/T790M/ACK1 to Overcome Osimertinib Resistance in Nonsmall Cell Lung Cancers

A Wang, W Shuai, C Wu, J Pei, P Yang… - Journal of Medicinal …, 2024 - ACS Publications
Activation of the alternative pathways and abnormal signaling transduction are frequently
observed in third-generation EGFR-TKIs (epidermal growth factor receptor tyrosine kinase …

Epidermal growth factor receptor dual-target inhibitors as a novel therapy for cancer: A review

C Wang, Y Zhang, T Zhang, J Xu, S Yan, B Liang… - International Journal of …, 2023 - Elsevier
Overexpression of the epidermal growth factor receptor (EGFR) has been linked to several
human cancers, including esophageal cancer, pancreatic cancer, anal cancer, breast …

Exploiting polypharmacology for improving therapeutic outcome of kinase inhibitors (KIs): An update of recent medicinal chemistry efforts

X Ma, X Lv, J Zhang - European Journal of Medicinal Chemistry, 2018 - Elsevier
Polypharmacology has been increasingly advocated for the therapeutic intervention in
complex pathological conditions, exemplified by cancer. Although kinase inhibitors (KIs) …

Synthesis, anticancer activity, toxicity evaluation and molecular docking studies of novel phenylaminopyrimidine—(thio) urea hybrids as potential kinase inhibitors

A Türe, DC Kahraman, R Cetin-Atalay… - … biology and chemistry, 2019 - Elsevier
Thirty-two novel urea/thiourea compounds as potential kinase inhibitor were designed,
synthesized and evaluated for their cytotoxic activity on breast (MCF7), colon (HCT116) and …

Investigation of the mechanisms of cytotoxic activity of 1, 3-disubstituted thiourea derivatives

P Strzyga-Łach, A Chrzanowska, K Podsadni… - Pharmaceuticals, 2021 - mdpi.com
Substituted thiourea derivatives possess confirmed cytotoxic activity towards cancer but also
normal cells. To develop new selective antitumor agents, a series of 3-(trifluoromethyl) …