Skip to main content
Journal cover image

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.

Publication ,  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.

Duke Scholars

Altmetric Attention Stats
Dimensions Citation Stats

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

APA
Chicago
ICMJE
MLA
NLM
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.
Journal cover image

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