On March 31, 2021, Wu, Xiaowei; Dai, Mengdi; Cui, Rongrong; Wang, Yulan; Li, Chunpu; Peng, Xia; Zhao, Jihui; Wang, Bao; Dai, Yang; Feng, Dan; Yang, Tianbiao; Jiang, Hualiang; Geng, Meiyu; Ai, Jing; Zheng, Mingyue; Liu, Hong published an article.Synthetic Route of 53724-96-2 The title of the article was Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyridazinone derivatives as covalent FGFR inhibitors. And the article contained the following:
Fibroblast growth factor receptors (FGFRs) have emerged as promising targets for anticancer therapy. In this study, we synthesized and evaluated the biol. activity of 66 pyrazolo[3,4-d]pyridazinone derivatives Kinase inhibition, cell proliferation, and whole blood stability assays were used to evaluate their activity on FGFR, allowing us to explore structure-activity relationships and thus to gain understanding of the structural requirements to modulate covalent inhibitors′ selectivity and reactivity. Among them, compound 10h exhibited potent enzymic activity against FGFR and remarkably inhibited proliferation of various cancer cells associated with FGFR dysregulation, and suppressed FGFR signaling pathway in cancer cells by the immunoblot anal. Moreover, 10h displayed highly potent antitumor efficacy (TGI = 91.6%, at a dose of 50 mg/kg) in the FGFR1-amplified NCI-H1581 xenograft model. The experimental process involved the reaction of Ethyl 6-methoxy-3-methylbenzofuran-2-carboxylate(cas: 53724-96-2).Synthetic Route of 53724-96-2
The Article related to pyrazolo pyridazinone derivative covalent fgfr inhibitor biol evaluation, pyridazinone derivative covalent fgfr inhibitor biol evaluation sar, antitumor efficacy, btk, brutons tyrosine kinase, cadd, computer-aided drug design, covalent fgfr inhibitors, egfr, epidermal growth factor receptor and other aspects.Synthetic Route of 53724-96-2
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem