Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.
Publication
, Journal Article
Feng, Y; Yin, Y; Weiser, A; Griffin, E; Cameron, MD; Lin, L; Ruiz, C; Schürer, SC; Inoue, T; Rao, PV; Schröter, T; Lograsso, P
Published in: J Med Chem
November 13, 2008
The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC 50 of approximately 3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.
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Published In
J Med Chem
DOI
EISSN
1520-4804
Publication Date
November 13, 2008
Volume
51
Issue
21
Start / End Page
6642 / 6645
Location
United States
Related Subject Headings
- rho-Associated Kinases
- Swine
- Structure-Activity Relationship
- Rats
- Pyrazoles
- Protein Kinase Inhibitors
- Molecular Structure
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Drug Evaluation, Preclinical
Citation
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Chicago
ICMJE
MLA
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Feng, Y., Yin, Y., Weiser, A., Griffin, E., Cameron, M. D., Lin, L., … Lograsso, P. (2008). Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem, 51(21), 6642–6645. https://doi.org/10.1021/jm800986w
Feng, Yangbo, Yan Yin, Amiee Weiser, Evelyn Griffin, Michael D. Cameron, Li Lin, Claudia Ruiz, et al. “Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.” J Med Chem 51, no. 21 (November 13, 2008): 6642–45. https://doi.org/10.1021/jm800986w.
Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, et al. Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem. 2008 Nov 13;51(21):6642–5.
Feng, Yangbo, et al. “Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.” J Med Chem, vol. 51, no. 21, Nov. 2008, pp. 6642–45. Pubmed, doi:10.1021/jm800986w.
Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P. Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem. 2008 Nov 13;51(21):6642–6645.
Published In
J Med Chem
DOI
EISSN
1520-4804
Publication Date
November 13, 2008
Volume
51
Issue
21
Start / End Page
6642 / 6645
Location
United States
Related Subject Headings
- rho-Associated Kinases
- Swine
- Structure-Activity Relationship
- Rats
- Pyrazoles
- Protein Kinase Inhibitors
- Molecular Structure
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Drug Evaluation, Preclinical