Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyridazinone derivatives as covalent FGFR inhibitors

Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyridazinone derivatives as covalent FGFR inhibitors

Fibroblast growth factor receptors (FGFRs) have emerged as promising targets for anticancer therapy. In this study, we synthesized and evaluated the biological activity of 66 pyrazolo[3,4-d]pyridazinone derivatives. Kinase inhibition, cell proliferation, and whole blood stability assays were used to...

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Bibliographic Details
Main Authors: Xiaowei Wu, Mengdi Dai, Rongrong Cui, Yulan Wang, Chunpu Li, Xia Peng, Jihui Zhao, Bao Wang, Yang Dai, Dan Feng, Tianbiao Yang, Hualiang Jiang, Meiyu Geng, Jing Ai, Mingyue Zheng, Hong Liu
Format: Article
Language:English
Published: Elsevier 2021-03-01
Series:Acta Pharmaceutica Sinica B
Subjects:
Tyrosine kinase
Covalent FGFR inhibitors
Virtual screening
Pyrazolo[3,4-d]pyridazinone
Structure−activity relationships
Antitumor efficacy
Online Access:http://www.sciencedirect.com/science/article/pii/S2211383520307024

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http://www.sciencedirect.com/science/article/pii/S2211383520307024

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