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 journal › Article

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 journal › Article

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.
@article{0d8e0cdcd94f46d9be5bb02187d7a111,
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.",
keywords = "Chromans, Glaucoma, Kinase, Rho kinase, ROCK, ROCK-II",
author = "Chen, {Yen Ting} and Bannister, {Thomas D.} and Amiee Weiser and Evelyn Griffin and Li Lin and Claudia Ruiz and Cameron, {Michael D.} and Schuerer, {Stephan C} and Derek Duckett and Thomas Schr{\"o}ter and Philip LoGrasso and Yangbo Feng",
year = "2008",
month = "12",
day = "15",
doi = "10.1016/j.bmcl.2008.10.080",
language = "English",
volume = "18",
pages = "6406--6409",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "24",

}

TY - JOUR

T1 - Chroman-3-amides as potent Rho kinase inhibitors

AU - Chen, Yen Ting

AU - Bannister, Thomas D.

AU - Weiser, Amiee

AU - Griffin, Evelyn

AU - Lin, Li

AU - Ruiz, Claudia

AU - Cameron, Michael D.

AU - Schuerer, Stephan C

AU - Duckett, Derek

AU - Schröter, Thomas

AU - LoGrasso, Philip

AU - Feng, Yangbo

PY - 2008/12/15

Y1 - 2008/12/15

N2 - 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.

AB - 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.

KW - Chromans

KW - Glaucoma

KW - Kinase

KW - Rho kinase

KW - ROCK

KW - ROCK-II

UR - http://www.scopus.com/inward/record.url?scp=56249104835&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=56249104835&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2008.10.080

DO - 10.1016/j.bmcl.2008.10.080

M3 - Article

C2 - 18990570

AN - SCOPUS:56249104835

VL - 18

SP - 6406

EP - 6409

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 24

ER -

Access to Document