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

doi:10.1016/j.bmcl.2008.10.080

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 journal › Article

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 language	English (US)
Pages (from-to)	6406-6409
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	24
DOIs	https://doi.org/10.1016/j.bmcl.2008.10.080
State	Published - Dec 15 2008
Externally published	Yes

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

Access to Document

10.1016/j.bmcl.2008.10.080

Fingerprint Dive into the research topics of 'Chroman-3-amides as potent Rho kinase inhibitors'. Together they form a unique fingerprint.

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

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.; Schürer, Stephan; 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

@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 Stephan Sch{\"u}rer and Derek Duckett and Thomas Schr{\"o}ter and Philip LoGrasso and Yangbo Feng",

year = "2008",

month = dec,

day = "15",

doi = "10.1016/j.bmcl.2008.10.080",

language = "English (US)",

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 - Schürer, Stephan

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 -