Send to

Choose Destination
See comment in PubMed Commons below
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.

Author information

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


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.

[PubMed - indexed for MEDLINE]

LinkOut - more resources

Full Text Sources

Chemical Information

PubMed Commons home

PubMed Commons

How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Write to the Help Desk