title: Chroman-3-amides as potent Rho kinase inhibitors.
abstract: Inhibition of Rho kinase (ROCK) is an attractive strategy for the treatment of diseases such as hypertension, glaucoma, and cancer. Here we report chroman-3-amides as highly potent ROCK inhibitors with sufficient kinase selectivity, excellent cell activity, good microsomal stability, and desirable pharmacokinetic properties for study as potential therapeutic agents.
authors.affiliation: Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, USA.
authors.forename: Yen Ting
authors.initials: YT
authors.lastname: Chen
authors.forename: Thomas D
authors.initials: TD
authors.lastname: Bannister
authors.forename: Amiee
authors.initials: A
authors.lastname: Weiser
authors.forename: Evelyn
authors.initials: E
authors.lastname: Griffin
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: Stephan
authors.initials: S
authors.lastname: Schürer
authors.forename: Derek
authors.initials: D
authors.lastname: Duckett
authors.forename: Thomas
authors.initials: T
authors.lastname: Schröter
authors.forename: Philip
authors.initials: P
authors.lastname: LoGrasso
authors.forename: Yangbo
authors.initials: Y
authors.lastname: Feng
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002839:Chromans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D005901:Glaucoma / Q000188:drug therapy*; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D013997:Time Factors; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000577:Amides; D002839:Chromans; D047428:Protein Kinase Inhibitors; D054460:rho-Associated Kinases