title: Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors.
abstract: 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).
authors.affiliation: Translational Research Institute, The Scripps Research Institute, Scripps Florida, Jupiter, FL 33458, USA.
authors.forename: Xingang
authors.initials: X
authors.lastname: Fang
authors.forename: Yen Ting
authors.initials: YT
authors.lastname: Chen
authors.forename: E Hampton
authors.initials: EH
authors.lastname: Sessions
authors.forename: Sarwat
authors.initials: S
authors.lastname: Chowdhury
authors.forename: Tomas
authors.initials: T
authors.lastname: Vojkovsky
authors.forename: Yan
authors.initials: Y
authors.lastname: Yin
authors.forename: Jennifer R
authors.initials: JR
authors.lastname: Pocas
authors.forename: Wayne
authors.initials: W
authors.lastname: Grant
authors.forename: Thomas
authors.initials: T
authors.lastname: Schröter
authors.forename: Li
authors.initials: L
authors.lastname: Lin
authors.forename: Claudia
authors.initials: C
authors.lastname: Ruiz
authors.forename: Michael D
authors.initials: MD
authors.lastname: Cameron
authors.forename: Philip
authors.initials: P
authors.lastname: LoGrasso
authors.forename: Thomas D
authors.initials: TD
authors.lastname: Bannister
authors.forename: Yangbo
authors.initials: Y
authors.lastname: Feng
mesh_terms: D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors*
chemical_list: D047428:Protein Kinase Inhibitors; D052999:Quinazolinones; D054460:rho-Associated Kinases