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

Alaric J. Dyckman; Charles M. Langevine; Claude Quesnelle; James Kempson; Junqing Guo; Patrice Gill; Steven H. Spergel; Scott H. Watterson; Tianle Li; David S. Nirschl; Kathleen M. Gillooly; Mark A. Pattoli; Kim W. McIntyre; Laishun Chen; Murray McKinnon; John H. Dodd; Joel C. Barrish; James R. Burke; William J. Pitts

doi:10.1016/j.bmcl.2010.10.133

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

Alaric J. Dyckman, Charles M. Langevine, Claude Quesnelle, James Kempson, Junqing Guo, Patrice Gill, Steven H. Spergel, Scott H. Watterson, Tianle Li, David S. Nirschl, Kathleen M. Gillooly, Mark A. Pattoli, Kim W. McIntyre, Laishun Chen, Murray McKinnon, John H. Dodd, Joel C. Barrish, James R. Burke, William J. Pitts

Chemistry

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	383-386
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2010.10.133
State	Published - Jan 1 2011

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2010.10.133

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Dyckman, A. J., Langevine, C. M., Quesnelle, C., Kempson, J., Guo, J., Gill, P., Spergel, S. H., Watterson, S. H., Li, T., Nirschl, D. S., Gillooly, K. M., Pattoli, M. A., McIntyre, K. W., Chen, L., McKinnon, M., Dodd, J. H., Barrish, J. C., Burke, J. R., & 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. Bioorganic and Medicinal Chemistry Letters, 21(1), 383-386. https://doi.org/10.1016/j.bmcl.2010.10.133

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title = "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",

abstract = "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.",

author = "Dyckman, {Alaric J.} and Langevine, {Charles M.} and Claude Quesnelle and James Kempson and Junqing Guo and Patrice Gill and Spergel, {Steven H.} and Watterson, {Scott H.} and Tianle Li and Nirschl, {David S.} and Gillooly, {Kathleen M.} and Pattoli, {Mark A.} and McIntyre, {Kim W.} and Laishun Chen and Murray McKinnon and Dodd, {John H.} and Barrish, {Joel C.} and Burke, {James R.} and Pitts, {William J.}",

year = "2011",

month = jan,

day = "1",

doi = "10.1016/j.bmcl.2010.10.133",

language = "English (US)",

volume = "21",

pages = "383--386",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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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 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', Bioorganic and Medicinal Chemistry Letters, vol. 21, no. 1, pp. 383-386. https://doi.org/10.1016/j.bmcl.2010.10.133

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. / Dyckman, Alaric J.; Langevine, Charles M.; Quesnelle, Claude et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 21, No. 1, 01.01.2011, p. 383-386.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2

T2 - Synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis

AU - Dyckman, Alaric J.

AU - Langevine, Charles M.

AU - Quesnelle, Claude

AU - Kempson, James

AU - Guo, Junqing

AU - Gill, Patrice

AU - Spergel, Steven H.

AU - Watterson, Scott H.

AU - Li, Tianle

AU - Nirschl, David S.

AU - Gillooly, Kathleen M.

AU - Pattoli, Mark A.

AU - McIntyre, Kim W.

AU - Chen, Laishun

AU - McKinnon, Murray

AU - Dodd, John H.

AU - Barrish, Joel C.

AU - Burke, James R.

AU - Pitts, William J.

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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

Abstract

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