Chroman-3-amides as potent Rho kinase inhibitors

Yen Ting Chen, Thomas D. Bannister, Amiee Weiser, Evelyn Griffin, Li Lin, Claudia Ruiz, Michael D. Cameron, Stephan Schürer, Derek Duckett, Thomas Schröter, Philip LoGrasso, Yangbo Feng

Research output: Contribution to journalArticle

42 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)6406-6409
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number24
DOIs
StatePublished - Dec 15 2008
Externally publishedYes

Keywords

  • Chromans
  • Glaucoma
  • Kinase
  • Rho kinase
  • ROCK
  • ROCK-II

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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  • Cite this

    Chen, Y. T., Bannister, T. D., Weiser, A., Griffin, E., Lin, L., Ruiz, C., Cameron, M. D., Schürer, S., Duckett, D., Schröter, T., LoGrasso, P., & Feng, Y. (2008). Chroman-3-amides as potent Rho kinase inhibitors. Bioorganic and Medicinal Chemistry Letters, 18(24), 6406-6409. https://doi.org/10.1016/j.bmcl.2008.10.080