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Bioorg Med Chem Lett. 2013 Mar 15;23(6):1592-9. doi: 10.1016/j.bmcl.2013.01.109. Epub 2013 Jan 31.

Amino acid derived quinazolines as Rock/PKA inhibitors.

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  • 1Medicinal Chemistry, Translational Research Institute, The Scripps Research Institute, 130 Scripps Way, 2A1, Jupiter, FL 33458, USA.

Abstract

SAR and lead optimization studies for Rock inhibitors based on amino acid-derived quinazolines are described. Studies demonstrated that these amino acid derived quinazolinones were mainly pan-Rock (I & II) inhibitors. While selectivity against other kinases could be achieved, selectivity for most of these compounds against PKA was not achieved. This is distinct from Rock inhibitors based on non-amino acid derived quinazolinones, where high selectivity against PKA could be obtained.(22) The inhibitors presented here in some cases possessed sub-nanomolar inhibition of Rock, nanomolar potency in ppMLC cell based assays, low to fair cytochrome P-450 inhibition, and good human microsomal stability.

Copyright © 2013 Elsevier Ltd. All rights reserved.

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