Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.
Publication
, Journal Article
Dyckman, AJ; Langevine, CM; Quesnelle, C; Kempson, J; Guo, J; Gill, P; Spergel, SH; Watterson, SH; Li, T; Nirschl, DS; Gillooly, KM; Chen, L ...
Published in: Bioorg Med Chem Lett
January 1, 2011
The synthesis, structure-activity relationships (SAR) and biological evaluation of thiazole based tricyclic inhibitors of IKK2 are described. Compound 9 was determined to be orally efficacious in a murine model of rheumatoid arthritis.
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Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
January 1, 2011
Volume
21
Issue
1
Start / End Page
383 / 386
Location
England
Related Subject Headings
- Thiazoles
- Structure-Activity Relationship
- Rats
- Pyridines
- Protein Kinase Inhibitors
- Mice, Inbred BALB C
- Mice
- Medicinal & Biomolecular Chemistry
- Imidazoles
- I-kappa B Kinase
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APA
Chicago
ICMJE
MLA
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Dyckman, A. J., Langevine, C. M., Quesnelle, C., Kempson, J., Guo, J., Gill, P., … Pitts, W. J. (2011). Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis. Bioorg Med Chem Lett, 21(1), 383–386. https://doi.org/10.1016/j.bmcl.2010.10.133
Dyckman, Alaric J., Charles M. Langevine, Claude Quesnelle, James Kempson, Junqing Guo, Patrice Gill, Steven H. Spergel, et al. “Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.” Bioorg Med Chem Lett 21, no. 1 (January 1, 2011): 383–86. https://doi.org/10.1016/j.bmcl.2010.10.133.
Dyckman AJ, Langevine CM, Quesnelle C, Kempson J, Guo J, Gill P, et al. Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis. Bioorg Med Chem Lett. 2011 Jan 1;21(1):383–6.
Dyckman, Alaric J., et al. “Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.” Bioorg Med Chem Lett, vol. 21, no. 1, Jan. 2011, pp. 383–86. Pubmed, doi:10.1016/j.bmcl.2010.10.133.
Dyckman AJ, Langevine CM, Quesnelle C, Kempson J, Guo J, Gill P, Spergel SH, Watterson SH, Li T, Nirschl DS, Gillooly KM, Pattoli MA, McIntyre KW, Chen L, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ. Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis. Bioorg Med Chem Lett. 2011 Jan 1;21(1):383–386.
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
January 1, 2011
Volume
21
Issue
1
Start / End Page
383 / 386
Location
England
Related Subject Headings
- Thiazoles
- Structure-Activity Relationship
- Rats
- Pyridines
- Protein Kinase Inhibitors
- Mice, Inbred BALB C
- Mice
- Medicinal & Biomolecular Chemistry
- Imidazoles
- I-kappa B Kinase