ArticleACS medicinal chemistry letters2025
Discovery of Reversible, Noncovalent Bruton's Tyrosine Kinase Inhibitors Targeting BTK C481S Mutation.
Article in ACS medicinal chemistry letters, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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2 citing papers in PubMed.
- Design, synthesis, and biological evaluation of novel isobenzofuran-1(3H)-one derivatives with antioxidant properties and improved oral bioavailability.Molecular diversity · 2026Article
- Special Issue: Antibody Therapy for Hematologic Malignancies.International journal of molecular sciences · 2025Article
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11 authors.
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Abstract
Bruton's tyrosine kinase (BTK) is a promising target for treatment of B-cell malignancies and autoimmune disorders. Application of first- and second-generation irreversible BTK inhibitors against various lymphomas and leukemia is well-known. Some clinical limitations, such as off-target toxicity and primary or acquired drug resistance mutations including BTK C481S have been observed for irreversible BTK inhibitors. Developing selective reversible, noncovalent BTK inhibitors is a suitable strategy to overcome drug resistance problems. Recent approval of pirtobrutinib by the FDA in 2023 stimulated research interests for developing noncovalent mutant selective BTK inhibitors. In this letter, we report the discovery of a novel series of 1
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