AI Article Synopsis
- Researchers focused on creating reversible and selective BTK inhibitors, using 7H-pyrrolo[2,3-d]pyrimidine and 1H-pyrrolo[2,3-b]pyridine as core structures.
- They found two promising lead compounds, 11 and 13, that showed strong BTK inhibition in various cell tests and high selectivity among 50 diverse kinases.
- These compounds also displayed good pharmacokinetics in mice and had positive effects in a mouse model for arthritis.
Article Abstract
In a pursuit to identify reversible and selective BTK inhibitors, two series based on 7H-pyrrolo[2,3-d]pyrimidine and 1H-pyrrolo[2,3-b]pyridine as the hinge binding core, have been identified. Structure activity relationship (SAR) exploration led to identification of two advanced lead molecules, 11 and 13, which demonstrated desired BTK inhibitory potency in different cellular assays, excellent selectivity in a panel of 50 diverse kinases, favorable in vivo PK properties in mice and anti-arthritic effect in a mouse model of CIA.
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| http://dx.doi.org/10.1016/j.bmcl.2017.02.026 | DOI Listing |
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