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• W3202521164 endingPage "128409" @default.
• W3202521164 startingPage "128409" @default.
• W3202521164 abstract "Tropomyosin receptor kinases (TRKA, TRKB, TRKC) are transmembrane receptor tyrosine kinases, which are respectively encoded by NTRK1, NTRK2, and NTRK3 genes. Herein, we reported the design, synthesis and Structure-Activity Relationship (SAR) investigation of a series of macrocyclic derivatives as new TRK inhibitors. Among these compounds, compound 9e exhibited strong kinase inhibitory activity (TRKG595R IC50 = 13.1 nM) and significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM) and compound 9e has shown a better inhibitory effect (IC50 = 0.646 μM) than control drug LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line. These results indicate that compound 9e is a potential TRK inhibitor for further investigation." @default.
• W3202521164 created "2021-10-11" @default.
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• W3202521164 date "2021-12-01" @default.
• W3202521164 modified "2023-09-23" @default.
• W3202521164 title "Design, synthesis and biological evaluation of macrocyclic derivatives as TRK inhibitors" @default.
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• W3202521164 doi "https://doi.org/10.1016/j.bmcl.2021.128409" @default.
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