Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 4803-74-1, Name is 5,6-Dimethoxy-2-(pyridin-4-ylmethylene)-2,3-dihydro-1H-inden-1-one, molecular formula is C17H15NO3, belongs to pyridine-derivatives compound, is a common compound. In a patnet, author is Krajcovicova, Sona, once mentioned the new application about 4803-74-1, Safety of 5,6-Dimethoxy-2-(pyridin-4-ylmethylene)-2,3-dihydro-1H-inden-1-one.
1,4,6-Trisubstituted imidazo[4,5-c]pyridines as inhibitors of Bruton’s tyrosine kinase
Herein, we report an efficient synthetic approach towards trisubstituted imidazo [4,5-clpyridines designed as inhibitors of Bruton’s tyrosine kinase (BTK). Two alternative synthetic routes for the simple preparation of desired compounds with variable substitutions at the N-1, C-4, C-6 positions were introduced with readily available building blocks. Further, the developed synthetic approach was feasible for isomeric compounds bearing imidazo [4,5-b]pyridine scaffolds. In contrast to expectations based on previous studies, the imidazo [4,5-c]pyridine inhibitor exhibited a significantly higher activity against BTK compared to its imidazo [4,5-b]pyridine isomer. An inherent SAR study in the series of imidazo [4,5-c]pyridine compounds revealed a remarkably high tolerance of C-6 substitutions for both hydrophobic and hydrophilic substituents. Preliminary cellular experiments indicated selective BTK targeting in Burkitt lymphoma and mantle cell lymphoma cell lines. The inhibitors could thus serve as starting points for further development, eventually leading to BTK inhibitors that could be used after ibrutinib failure. (C) 2020 Elsevier Masson SAS. All rights reserved.
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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem