.png){kind=icon}
.png){kind=icon}
Return
Design of fibroblast growth factor receptor (FGFR) inhibitors containing a 3,4-dihydropyrido[4,3-d]pyrimidin-2(1H)-one motif
.png){kind=icon}
PRE
AI
Y
Z
Y
J
Y
H
H
S
DOI：10.1016/j.ejmech.2026.118912.png)
.png){kind=icon}
Original request for help.png){kind=icon}
Share.png){kind=icon}
Save
Abstract
En 中文
• Structural modification of BGJ398 yielded compound 1a with superior antiproliferative potency. • Compound 1a exhibits balanced, broad-spectrum FGFR1-4 inhibition, outperforming clinically approved erdafitinib in FGFR4 activity • 1a shows high oral bioavailability (66.9%) and favorable pharmacokinetic properties in CD-1 mice. • 1a can induce cellular ferroptosis, which is a unique feature that enhances its antitumor potential.
Keywords:
FGFR inhibitors
structural modification
antiproliferative potency
ferroptosis
pharmacokinetics
Journal
IF:
5.9
Papers:
1.7W
Citations:
6.0W
Organization
Cited Papers