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Structure-Based Design of 2-Aminopyrazolpyrimidopyridone Derivatives as New Rearranged During Transfection (RET) Kinase Inhibitors.

Chemical biology & drug design - 1 Jan 2025

Shen Jiayi, Liu Jihu, Tan Zhiyong, Li Anzhi, Chen Sheng, Li Yongdong

Abstract excerpt

RET (Rearranged during transfection) kinase is a validated target for non-small cell lung cancer (NSCLC). In 2020, two selective RET inhibitors, selpercatinib and pralsetinib were approved by the US FDA. However, high treatment costs and clinically acquired resistance (e.g., G810C/S/R) become the new challenges for RET-based therapies. In this work, we discovered a series of 2-aminopyrazolpyrimidopyridone RET...

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PMID: 39739433
DOI: 10.1111/cbdd.70039

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Structure-Based Design of 2-Aminopyrazolpyrimidopyridone Derivatives as New Rearranged During Transfection (RET) Kinase Inhibitors.PMID 39739433Read ↗

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