| Structural highlights
Publication Abstract from PubMed
We report the SAR around a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency but moderate kinase selectivity, while 2-aminobenzyl analogs that fill the Ala571 subpocket exhibit good inhibition activity and excellent kinase selectivity.
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.,Powell NA, Hoffman JK, Ciske FL, Kaufman MD, Kohrt JT, Quin J 3rd, Sheehan DJ, Delaney A, Baxi SM, Catana C, McConnell P, Ohren J, Perrin LA, Edmunds JJ Bioorg Med Chem Lett. 2013 Feb 15;23(4):1046-50. doi: 10.1016/j.bmcl.2012.12.013., Epub 2012 Dec 20. PMID:23312472[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Powell NA, Hoffman JK, Ciske FL, Kaufman MD, Kohrt JT, Quin J 3rd, Sheehan DJ, Delaney A, Baxi SM, Catana C, McConnell P, Ohren J, Perrin LA, Edmunds JJ. Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1046-50. doi: 10.1016/j.bmcl.2012.12.013., Epub 2012 Dec 20. PMID:23312472 doi:http://dx.doi.org/10.1016/j.bmcl.2012.12.013
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