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 › peer-review

44 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

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10.1016/j.bmcl.2008.10.080

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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 › peer-review

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AU - Weiser, Amiee

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AU - Ruiz, Claudia

AU - Cameron, Michael D.

AU - Schürer, Stephan

AU - Duckett, Derek

AU - Schröter, Thomas

AU - LoGrasso, Philip

AU - Feng, Yangbo

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