Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer
Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer
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吲唑衍生物的设计、合成和生物学评价作为选择性和有效的 FGFR4 抑制剂，用于治疗 FGF19 驱动的肝细胞癌
DOI：
10.1016/j.ejmech.2021.113219
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发表时间：
2021-02-19
影响因子：
6.7
通讯作者：
Cai, Yuepiao
中科院分区：
文献类型：
--
作者：
Chen, Xiaolu;Liu, Yanan;Cai, Yuepiao
Fibroblast growth factor receptor 4 (FGFR4) is a member of the fibroblast growth factor receptor family, which is closely related to the occurrence and development of hepatocellular carcinoma (HCC). In this article, a series of indazole derivatives were designed and synthesized by using computer-aided drug design (CADD) and structure-based design strategies, and then they were evaluated for their inhibition of FGFR4 kinase and antitumor activity. F-30 was subtly selective for FGFR4 compared to FGFR1; it affected cell growth and migration by inhibiting FGFR4 pathways in HCC cell lines in a dose-dependent manner. (C) 2021 Elsevier Masson SAS. All rights reserved.
