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Article

A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.

Journal of medicinal chemistry - 14 Jan 2016

Yoon Hojong, Kwak Yeonui, Choi Seunghye, Cho Hanna, Kim Nam Doo, Sim Taebo

Abstract excerpt

Aberrant RET kinase signaling plays critical roles in several human cancers such as thyroid carcinoma. The gatekeeper mutants (V804L or V804M) of RET are resistant to currently approved RET inhibitors such as cabozantinib and vandetanib. We, for the first time, report a highly selective and extremely potent RET inhibitor, 6i rationally designed. Compound 6i inhibits strongly RET gatekeeper mutants and other...

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Identifiers

PMID: 26652860
DOI: 10.1021/acs.jmedchem.5b01522

Genes

RET

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.PMID 26652860Read ↗

Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant.Semantic proximity Read ↗

Identification of a novel 5-amino-3-(5-cyclopropylisoxazol-3-yl)-1-isopropyl-1H-pyrazole-4-carboxamide as a specific RET kinase inhibitor.Semantic proximity Read ↗

Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors.Semantic proximity Read ↗

Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose.Semantic proximity Read ↗

Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.Semantic proximity Read ↗

Systematic Analysis of Tyrosine Kinase Inhibitor Response to RET Gatekeeper Mutations in Thyroid Cancer.Semantic proximity Read ↗

Discovery of CN-3 as a Next-Generation RET Inhibitor Potently Overcoming Multiple Mutations.Semantic proximity Read ↗

Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase.Semantic proximity Read ↗

Discovery of wt RET and V804M RET Inhibitors: From Hit to Lead.Semantic proximity Read ↗

Identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascadeSemantic proximity Read ↗

RET kinase inhibitors: a review of recent patents (2012–2015)Semantic proximity Read ↗

Targeting RET alterations in cancer: Recent progress and future directions.Semantic proximity Read ↗

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