AI Article Synopsis
- * One compound displayed significant cytotoxicity against NSCLC cells (A549 and H460), proving to be more effective than the chemotherapy drug cisplatin.
- * Previous studies confirmed that these compounds target the epidermal growth factor receptor (EGFR), which is crucial in NSCLC treatment, with further analyses showing the ability of the compound to bind stably to EGFR.
Article Abstract
A series of amino acid ester trifluoroacetate derivatives was synthesized from scaberol C. They were screened for their inhibitory activity against Non-Small Cell Lung Cancer (NSCLC) cells. Among them, compound showed significant cytotoxicity against A549 and H460 cells (IC), and was more active than cisplatin (DDP). The epidermal growth factor receptor (EGFR) was overexpressed in NSCLC, which was the target of multiple cancer therapies and a strong prognostic indicator. Our previous studies reported that the target of scaberol C derivatives against NSCLC cells was EGFR. And then molecular docking analysis and molecular dynamics (MD) simulations indicated that can stably and covalently bind to the EGFR target protein.
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| http://dx.doi.org/10.1080/10286020.2024.2380737 | DOI Listing |
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