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• W2891239180 endingPage "3311" @default.
• W2891239180 startingPage "3307" @default.
• W2891239180 abstract "Bruton's tyrosine kinase (Btk) is a member of the Tec kinase family that is expressed in cells of hematopoietic lineage (e.g. B cells, macrophages, monocytes, and mast cells). Small molecule covalent irreversible Btk inhibitors targeting Cys481 within the ATP-binding pocket have been applied in the treatment of B-cell malignancies. Starting from a fragment, we discovered a novel series of potent covalent irreversible Btk inhibitors that bear N-linked groups occupying the solvent accessible pocket (SAP) of the active site of the Btk kinase domain. The hit molecules, however, displayed high P-gp mediated efflux ratio (ER) and poor A-B permeability in Caco-2 assay. By decreasing tPSA, installing steric hindrance and adjusting clogP, one top molecule 9 was discovered, which showed a 99% decrease in efflux ratio and a 90-fold increase in A-B permeability compared to hit molecule 1." @default.
• W2891239180 created "2018-09-27" @default.
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• W2891239180 date "2018-11-01" @default.
• W2891239180 modified "2023-09-24" @default.
• W2891239180 title "Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors" @default.
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• W2891239180 doi "https://doi.org/10.1016/j.bmcl.2018.09.018" @default.
• W2891239180 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30243592" @default.
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