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Published in 2018 at "Cancer Medicine"
DOI: 10.1002/cam4.1392
Abstract: YL143 was identified as a novel wild‐type sparing EGFRT790M inhibitor with good pharmacokinetic properties. It potently suppresses EGFRL858R/T790M with an 50% inhibitory concentration (IC50) value of 2.0 ± 0.3 nmol/L, but is approximately 92‐folds less…
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Keywords:
yl143;
inhibitor;
novel mutant;
egfrl858r t790m ... See more keywords
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Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.11.069
Abstract: Third-generation epidermal growth factor receptor (EGFR)L858R/T790M inhibitors are still the main drugs for the treatment of advanced non-small cell lung cancer (NSCLC), and these drugs have achieved remarkable clinical efficacy. However, there are still many…
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Keywords:
design synthesis;
t790m inhibitors;
t790m;
egfrl858r t790m ... See more keywords
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Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.113019
Abstract: Lung cancer is the leading cause of cancer deaths. It has been demonstrated that epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKI) are efficacious in patients with EGFR mutation-positive non-small cell lung cancer (NSCLC). In…
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Keywords:
selective egfrl858r;
pyrimidine derivatives;
diaryl pyrimidine;
egfrl858r t790m ... See more keywords
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3
Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.1c00651
Abstract: Target identification is an essential step in drug discovery. It facilitates an understanding of drug action and potential toxicities and offers opportunities to repurpose drug candidates. HP-1, a potent EGFRL858R/T790M (epidermal growth factor receptor) mutant…
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Keywords:
mutant inhibitor;
egfrl858r t790m;
potent egfrl858r;
identification ... See more keywords
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Published in 2023 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2023.2205605
Abstract: Abstract EGFR mutations have been identified in 20,000 reported NSCLC (non-small cell lung cancer) samples, and exon 19 deletions and L858R mutations at position 21, known as “classical” mutations, account for 85–90% of the total…
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Keywords:
design synthesis;
synthesis biological;
biological evaluation;
egfrl858r t790m ... See more keywords