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Abstract #28035 Published in IGR 13-1
Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors
Fang X; Chen YT; Sessions EH; Chowdhury S; Vojkovsky T; Yin Y; Pocas JR; Grant W; Schroter T; Lin LBioorganic and Medicinal Chemistry Letters 2011; 21:1844-1848
Rho kinase (ROCK) is an attractive therapeutic target for various diseases including glaucoma, hypertension, and spinal cord injury. Herein, we report the development of a series of ROCK-II inhibitors based on 4-quinazolinone and quinazoline scaffolds. SAR studies at three positions of the quinazoline core led to the identification of analogs with high potency against ROCK-II and good selectivity over protein kinase A (PKA). (copyright) 2011 Elsevier Ltd. All rights reserved.
Y.T. Chen. Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Inst, . ytchen@scripps.edu
Classification:
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)
3.8 Pharmacology (Part of: 3 Laboratory methods)
