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 C Schuerer, Derek Duckett, Thomas Schröter, Philip LoGrasso, Yangbo Feng

Research output: Contribution to journalArticle

39 Citations (Scopus)

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

Fingerprint

Chromans
rho-Associated Kinases
Pharmacokinetics
Amides
Glaucoma
Phosphotransferases
Hypertension
Neoplasms
Therapeutics

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

Cite this

Chen, Y. T., Bannister, T. D., Weiser, A., Griffin, E., Lin, L., Ruiz, C., ... 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

Chroman-3-amides as potent Rho kinase inhibitors. / Chen, Yen Ting; Bannister, Thomas D.; Weiser, Amiee; Griffin, Evelyn; Lin, Li; Ruiz, Claudia; Cameron, Michael D.; Schuerer, Stephan C; Duckett, Derek; Schröter, Thomas; LoGrasso, Philip; Feng, Yangbo.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 18, No. 24, 15.12.2008, p. 6406-6409.

Research output: Contribution to journalArticle

Chen, YT, Bannister, TD, Weiser, A, Griffin, E, Lin, L, Ruiz, C, Cameron, MD, Schuerer, SC, Duckett, D, Schröter, T, LoGrasso, P & Feng, Y 2008, 'Chroman-3-amides as potent Rho kinase inhibitors', Bioorganic and Medicinal Chemistry Letters, vol. 18, no. 24, pp. 6406-6409. https://doi.org/10.1016/j.bmcl.2008.10.080
Chen YT, Bannister TD, Weiser A, Griffin E, Lin L, Ruiz C et al. Chroman-3-amides as potent Rho kinase inhibitors. Bioorganic and Medicinal Chemistry Letters. 2008 Dec 15;18(24):6406-6409. https://doi.org/10.1016/j.bmcl.2008.10.080
Chen, Yen Ting ; Bannister, Thomas D. ; Weiser, Amiee ; Griffin, Evelyn ; Lin, Li ; Ruiz, Claudia ; Cameron, Michael D. ; Schuerer, Stephan C ; Duckett, Derek ; Schröter, Thomas ; LoGrasso, Philip ; Feng, Yangbo. / Chroman-3-amides as potent Rho kinase inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2008 ; Vol. 18, No. 24. pp. 6406-6409.
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