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September 5, 2025Journal of Medicinal Chemistry

Direct Ser797 Interacted Pteridine-7(8H)-one Derivatives as Highly Selective and Orally Available EGFRL858R/T790M/C797S Inhibitors

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Authors

WJWenzhe JiangYHYongning HeYWYongxiang Wang

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Overview

Developed pteridine derivatives inhibit EGFRL858R/T790M/C797S, indicating a potential strategy against osimertinib resistance.

Key Points

  • M49 showed potent inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 18.94 nM.
  • Pharmacokinetic studies indicated that M49 had a Cmax of 230.07 ng/mL after 10 mg/kg oral dosing.
  • In xenograft models, M49 demonstrated a tumor growth inhibition rate of 73.53% compared to 56.05% for Brigatinib.
  • This research highlights a novel discovery strategy for EGFRL858R/T790M/C797S inhibitors using pteridin-7(8H)-one derivatives.

Cite This Study

Jiang et al. (2025) studied this question.

synapsesocial.com/papers/68c238d2b210217d64778b3ahttps://doi.org/10.1021/acs.jmedchem.5c01313
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