Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis
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W Zhang, AL McIver, MA Stashko…
Journal of medicinal …, 2013
ACS Publications
The role of Mer kinase in regulating the second phase of platelet activation generates an opportunity to use Mer inhibitors for preventing thrombosis with diminished likelihood for bleeding as compared to current therapies. Toward this end, we have discovered a novel, Mer kinase specific substituted-pyrimidine scaffold using a structure-based drug design and a pseudo ring replacement strategy. The cocrystal structure of Mer with two compounds (7 and 22) possessing distinct activity have been determined. Subsequent SAR studies …
