16019-31-1Relevant articles and documents
ATROPISOMERISM FOR ENHANCED KINASE INHIBITOR SELECTIVITY
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Page/Page column 33, (2019/01/10)
The invention provides a series of conformationally stable and selective kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly inter
Exploiting Atropisomerism to Increase the Target Selectivity of Kinase Inhibitors
Smith, Davis E.,Marquez, Isaac,Lokensgard, Melissa E.,Rheingold, Arnold L.,Hecht, David A.,Gustafson, Jeffrey L.
supporting information, p. 11754 - 11759 (2015/10/05)
Many biologically active molecules exist as rapidly interconverting atropisomeric mixtures. Whereas one atropisomer inhibits the desired target, the other can lead to off-target effects. Herein, we study atropisomerism as a possibility to improve the sele
A ring-closing metathesis approach to heterocycle-fused azepines
Moss, Thomas A.
supporting information, p. 993 - 997 (2013/03/28)
Heterocycle-fused azepines, an important class of molecular scaffold, are readily synthesised through the ruthenium-catalysed ring-closing metathesis reaction. Although benzo-fused azepines are well documented, heterocycle-fused examples are poorly developed. Herein, a range of five- and six-membered heterocycle-fused azepines are investigated, allowing access to a series of pharmaceutically interesting products.