Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.
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, Journal Article
Kempson, J; Guo, J; Das, J; Moquin, RV; Spergel, SH; Watterson, SH; Langevine, CM; Dyckman, AJ; Pattoli, M; Burke, JR; Yang, X; Gillooly, KM ...
Published in: Bioorg Med Chem Lett
May 15, 2009
A new series of tricyclic-based inhibitors of IKK have been derived from an earlier lead compound. The synthesis and structure-activity relationships (SAR) are described. Compound 4k inhibited TNF production in rats stimulated with LPS.
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Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
May 15, 2009
Volume
19
Issue
10
Start / End Page
2646 / 2649
Location
England
Related Subject Headings
- Tumor Necrosis Factor-alpha
- Structure-Activity Relationship
- Rats
- Pyrimidines
- Protein Kinase Inhibitors
- Medicinal & Biomolecular Chemistry
- Lipopolysaccharides
- Imidazoles
- I-kappa B Kinase
- Animals
Citation
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Chicago
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Kempson, J., Guo, J., Das, J., Moquin, R. V., Spergel, S. H., Watterson, S. H., … Pitts, W. J. (2009). Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase. Bioorg Med Chem Lett, 19(10), 2646–2649. https://doi.org/10.1016/j.bmcl.2009.03.159
Kempson, James, Junqing Guo, Jagabandhu Das, Robert V. Moquin, Steven H. Spergel, Scott H. Watterson, Charles M. Langevine, et al. “Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.” Bioorg Med Chem Lett 19, no. 10 (May 15, 2009): 2646–49. https://doi.org/10.1016/j.bmcl.2009.03.159.
Kempson J, Guo J, Das J, Moquin RV, Spergel SH, Watterson SH, et al. Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase. Bioorg Med Chem Lett. 2009 May 15;19(10):2646–9.
Kempson, James, et al. “Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.” Bioorg Med Chem Lett, vol. 19, no. 10, May 2009, pp. 2646–49. Pubmed, doi:10.1016/j.bmcl.2009.03.159.
Kempson J, Guo J, Das J, Moquin RV, Spergel SH, Watterson SH, Langevine CM, Dyckman AJ, Pattoli M, Burke JR, Yang X, Gillooly KM, McIntyre KW, Chen L, Dodd JH, McKinnon M, Barrish JC, Pitts WJ. Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase. Bioorg Med Chem Lett. 2009 May 15;19(10):2646–2649.
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
May 15, 2009
Volume
19
Issue
10
Start / End Page
2646 / 2649
Location
England
Related Subject Headings
- Tumor Necrosis Factor-alpha
- Structure-Activity Relationship
- Rats
- Pyrimidines
- Protein Kinase Inhibitors
- Medicinal & Biomolecular Chemistry
- Lipopolysaccharides
- Imidazoles
- I-kappa B Kinase
- Animals