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Design, synthesis and biological evaluation of pyrazolo[3,4-<i>b</i>]pyridine derivatives as TRK inhibitors

Nian Liu, Xin Wang, Qinglin Fu, Qiaohua Qin, Tianxiao Wu, Ruicheng Lv, Dongmei Zhao, Maosheng Cheng

2022RSC Medicinal Chemistry16 citationsDOIOpen Access PDF

Abstract

value of 0.304 μM together with obvious selectivity for the MCF-7 cell line and HUVEC cell line. Furthermore, compound C03 possessed good plasma stability and low inhibitory activity to a panel of cytochrome P450 isoforms except CYP2C9. Overall, C03 has potential for further exploration.

Topics & Concepts

Trk receptorPyridineChemistryCombinatorial chemistryStereochemistryBiochemistryOrganic chemistryReceptorNeurotrophinQuinazolinone synthesis and applicationsCytokine Signaling Pathways and InteractionsMelanoma and MAPK Pathways