Design, synthesis, and biological evaluation of quinazoline derivatives with covalent reversible warheads as potential FGFR4 inhibitors

[Display omitted] •A series of quinazoline derivatives designed to covalent reversible binding with FGFR4.•Compound C3 displayed a certain FGFR4 inhibitory potency with an IC50 value of 0.42 ± 0.16 μM.•Compound C3 exhibited covalent reversible nature in binding mechanism study. Fibroblast growth fac...

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Veröffentlicht in:	Bioorganic chemistry 2022-04, Vol.121, p.105673-105673, Article 105673
Hauptverfasser:	Nie, Wenwen, Lu, Yang, Pan, Chenghao, Gao, Jian, Luo, Mengxin, Du, Jiaming, Wang, Jiao, Luo, Peihua, Zhu, Hong, Che, Jinxin, He, Qiaojun, Dong, Xiaowu
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-tumor Carcinoma, Hepatocellular - drug therapy Cell Line, Tumor Cell Proliferation Covalent reversible FGFR4 inhibitor Humans Liver Neoplasms - drug therapy Quinazolines - pharmacology Quinazolines - therapeutic use Receptor, Fibroblast Growth Factor, Type 4 - chemistry Receptor, Fibroblast Growth Factor, Type 4 - metabolism
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