Organic & Biomolecular Chemistry · 2024 · 14 citations · 25 references
PharmacyMedicinal ChemistryPharmacologyCancer PharmacologyDrug DiscoveryStructure-activity RelationshipsCovalent Drug DesignCovalent Inhibitor DesignCytotoxic ChemotherapyEnzyme InhibitionLead Compound DesignScaffold HoppingAnticancer ActivityBioactivityBioactivity AssessmentBioactivity ScreeningChemical Scaffold HoppingKras G12c InhibitionKras InhibitorsPyridine Chemistry
Novel imidazo[1,2- a ]pyridine-based covalent inhibitors were synthesized via the scaffold hopping strategy. In vitro bioactivity assessment concluded that I-11 is a potent and selective KRAS G12C inhibitor.
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K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions
J.M. Ostrem, Ulf Peters, Martin L. Sos et al. · Nature · 2013 · 2.5K citations · Full text
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Jude Canon, Karen Rex, Anne Y. Saiki et al. · Nature · 2019 · 2.3K citations
Medicine, Oncology, Pharmacology +14
KRAS <sup>G12C</sup> Inhibition with Sotorasib in Advanced Solid Tumors
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Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor
Matthew R. Janes, Jingchuan Zhang, Lian‐Sheng Li et al. · Cell · 2018 · 1.2K citations · Full text