YL143, a novel mutant selective irreversible EGFR inhibitor, overcomes EGFRL858R, T790M‐mutant resistance in vitro and in vivo
Sign Up to like & getrecommendations! 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… read more here.
Keywords: yl143; inhibitor; novel mutant; egfrl858r t790m ... See more keywords
Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFRL858R/T790M inhibitors.
Sign Up to like & getrecommendations! 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… read more here.
Keywords: design synthesis; t790m inhibitors; t790m; egfrl858r t790m ... See more keywords
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFRL858R/T790M inhibitors.
Sign Up to like & getrecommendations! 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… read more here.
Keywords: selective egfrl858r; pyrimidine derivatives; diaryl pyrimidine; egfrl858r t790m ... See more keywords
Proteome-wide Identification of Off-Targets of a Potent EGFRL858R/T790M Mutant Inhibitor.
Sign Up to like & getrecommendations! 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… read more here.
Keywords: mutant inhibitor; egfrl858r t790m; potent egfrl858r; identification ... See more keywords
Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidine and thieno[2,3-d]pyrimidine derivatives as novel EGFRL858R/T790M inhibitors
Sign Up to like & getrecommendations! 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… read more here.
Keywords: design synthesis; synthesis biological; biological evaluation; egfrl858r t790m ... See more keywords