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Updated: May 14, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Amino acid derived quinazolines as Rock/PKA inhibitors
Sarwat Chowdhury1, Yen Ting Chen, Xingang Fang
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.
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