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 H. Dodd; Murray McKinnon; Joel C. Barrish; William J. Pitts

doi: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

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 H. Dodd, Murray McKinnon, Joel C. Barrish, William J. Pitts

Chemistry

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

22 Scopus citations

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 language	English (US)
Pages (from-to)	2646-2649
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2009.03.159
State	Published - May 15 2009

All Science Journal Classification (ASJC) codes

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

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Kempson, J., Guo, J., Das, J., Moquin, R. V., Spergel, S. H., Watterson, S. H., Langevine, C. M., Dyckman, A. J., Pattoli, M., Burke, J. R., Yang, X. X., Gillooly, K. M., McIntyre, K. W., Chen, L., Dodd, J. H., McKinnon, M., Barrish, J. C., & 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 IκB kinase. Bioorganic and Medicinal Chemistry Letters, 19(10), 2646-2649. https://doi.org/10.1016/j.bmcl.2009.03.159

@article{e7eaed313dfe417fac3e67b7fd490fa3,

title = "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",

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 H.} and Murray McKinnon and Barrish, {Joel C.} and Pitts, {William J.}",

year = "2009",

month = may,

day = "15",

doi = "10.1016/j.bmcl.2009.03.159",

language = "English (US)",

volume = "19",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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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

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 H.

AU - McKinnon, Murray

AU - Barrish, Joel C.

AU - Pitts, William J.

PY - 2009/5/15

Y1 - 2009/5/15

N2 - 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.

AB - 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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AN - SCOPUS:65349119487

SN - 0960-894X

VL - 19

SP - 2646

EP - 2649

JO - Bioorganic and Medicinal Chemistry Letters

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IS - 10

ER -

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

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