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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10.1016/j.bmcl.2009.03.159

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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",

pages = "2646--2649",

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.

UR - https://www.scopus.com/pages/publications/65349119487

UR - https://www.scopus.com/pages/publications/65349119487#tab=citedBy

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DO - 10.1016/j.bmcl.2009.03.159

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AN - SCOPUS:65349119487

SN - 0960-894X

VL - 19

SP - 2646

EP - 2649

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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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