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

46 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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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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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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.",

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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

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JO - Bioorganic and Medicinal Chemistry Letters

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SN - 0960-894X

IS - 24

ER -

Chroman-3-amides as potent Rho kinase inhibitors

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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