Abstract:Developing selective inhibitors for Janus kinase 1 (JAK1)
is a
significant focus for improving the efficacy and alleviating the adverse
effects in treating immune–inflammatory diseases. Herein, we
report the discovery of a series of C-5 pyrazole-modified pyrrolopyrimidine
derivatives as JAK1-selective inhibitors. The potential hydrogen bond
between the pyrazole group and E966 in JAK1 is the key point that
enhances JAK1 selectivity. These compounds exhibit 10- to 20-fold
JAK1 selectivity over JAK2 in enzyme ass… Show more
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