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

• Main Authors: Xiaowei Wu (Author), Mengdi Dai (Author), Rongrong Cui (Author), Yulan Wang (Author), Chunpu Li (Author), Xia Peng (Author), Jihui Zhao (Author), Bao Wang (Author), Yang Dai (Author), Dan Feng (Author), Tianbiao Yang (Author), Hualiang Jiang (Author), Meiyu Geng (Author), Jing Ai (Author), Mingyue Zheng (Author), Hong Liu (Author)
• Format: Book
• Published: Elsevier, 2021-03-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...