Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IκB kinase

James Kempson, Junqing Guo, Jagabandhu Das, Robert V. Moquin, Steven H. Spergel, Scott H. Watterson, Charles M. Langevine, Alaric J. Dyckman, Mark Pattoli, James R. Burke, Xiao Xia Yang, Kathleen M. Gillooly, Kim W. McIntyre, Laishun Chen, John Harold Dodd, Murray McKinnon, Joel C. Barrish, William J. Pitts

Research output: Contribution to journalArticle

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Abstract

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.

Original languageEnglish (US)
Pages (from-to)2646-2649
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number10
DOIs
StatePublished - May 15 2009

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Lead compounds
Structure-Activity Relationship
Amines
Rats
Phosphotransferases
Lead

All Science Journal Classification (ASJC) codes

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

Cite this

Kempson, James ; Guo, Junqing ; Das, Jagabandhu ; Moquin, Robert V. ; Spergel, Steven H. ; Watterson, Scott H. ; Langevine, Charles M. ; Dyckman, Alaric J. ; Pattoli, Mark ; Burke, James R. ; Yang, Xiao Xia ; Gillooly, Kathleen M. ; McIntyre, Kim W. ; Chen, Laishun ; Dodd, John Harold ; McKinnon, Murray ; Barrish, Joel C. ; Pitts, William J. / Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IκB kinase. In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 10. pp. 2646-2649.
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abstract = "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.",
author = "James Kempson and Junqing Guo and Jagabandhu Das and Moquin, {Robert V.} and Spergel, {Steven H.} and Watterson, {Scott H.} and Langevine, {Charles M.} and Dyckman, {Alaric J.} and Mark Pattoli and Burke, {James R.} and Yang, {Xiao Xia} and Gillooly, {Kathleen M.} and McIntyre, {Kim W.} and Laishun Chen and Dodd, {John Harold} and Murray McKinnon and Barrish, {Joel C.} and Pitts, {William J.}",
year = "2009",
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doi = "10.1016/j.bmcl.2009.03.159",
language = "English (US)",
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Kempson, J, Guo, J, Das, J, Moquin, RV, Spergel, SH, Watterson, SH, Langevine, CM, Dyckman, AJ, Pattoli, M, Burke, JR, Yang, XX, Gillooly, KM, McIntyre, KW, Chen, L, Dodd, JH, McKinnon, M, Barrish, JC & Pitts, WJ 2009, 'Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IκB kinase', Bioorganic and Medicinal Chemistry Letters, vol. 19, no. 10, pp. 2646-2649. https://doi.org/10.1016/j.bmcl.2009.03.159

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IκB kinase. / Kempson, James; Guo, Junqing; Das, Jagabandhu; Moquin, Robert V.; Spergel, Steven H.; Watterson, Scott H.; Langevine, Charles M.; Dyckman, Alaric J.; Pattoli, Mark; Burke, James R.; Yang, Xiao Xia; Gillooly, Kathleen M.; McIntyre, Kim W.; Chen, Laishun; Dodd, John Harold; McKinnon, Murray; Barrish, Joel C.; Pitts, William J.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 10, 15.05.2009, p. 2646-2649.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IκB kinase

AU - Kempson, James

AU - Guo, Junqing

AU - Das, Jagabandhu

AU - Moquin, Robert V.

AU - Spergel, Steven H.

AU - Watterson, Scott H.

AU - Langevine, Charles M.

AU - Dyckman, Alaric J.

AU - Pattoli, Mark

AU - Burke, James R.

AU - Yang, Xiao Xia

AU - Gillooly, Kathleen M.

AU - McIntyre, Kim W.

AU - Chen, Laishun

AU - Dodd, John Harold

AU - McKinnon, Murray

AU - Barrish, Joel C.

AU - Pitts, William J.

PY - 2009/5/15

Y1 - 2009/5/15

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