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February 8, 2026

Structure-Based Design of 4-(1-Methyl-1H-indol-3-yl)pyrimidin-2-amine Derivatives as the First Covalent FGFR3 Selective Inhibitors.

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Authors

WZWenjian ZhuXCXiaojuan ChenXLXiaofei Li

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Overview

Reports the design of FGFR3 selective inhibitors showing efficacy against resistance mutations in bladder cancer, suggesting clinical potential.

Key Points

  • The aim is to create selective inhibitors for FGFR3 to combat resistance mutations in bladder cancer.
  • Utilized structure-based drug design for compound development
  • Tested potency against FGFR3 and other FGFR isoforms
  • Evaluated antiproliferative effects in bladder cancer cell lines
  • Assessed antitumor efficacy in a xenograft model
  • Compound 10s showed IC50 of 6.8 nM against FGFR3
  • Demonstrated 5-60 fold selectivity over FGFR1/2/4
  • Effective against FGFR3 V555M mutation with IC50 of 19.2 nM
  • Exhibited antiproliferative effects with IC50 of 9.2 nM in FGFR3-driven RT112/84 cells
  • Significant antitumor efficacy in bladder cancer xenograft model

Cite This Study

Zhu et al. (2026) studied this question.

synapsesocial.com/papers/698827f00fc35cd7a8846fcdhttps://doi.org/10.1021/acs.jmedchem.5c02552
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