Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors

Alaric J. Dyckman; Tianle Li; Sidney Pitt; Rosemary Zhang; Ding Ren Shen; Kim W. McIntyre; Kathleen M. Gillooly; David J. Shuster; Arthur M. Doweyko; John S. Sack; Kevin Kish; Susan E. Kiefer; John A. Newitt; Hongjian Zhang; Punit H. Marathe; Murray McKinnon; Joel C. Barrish; John H. Dodd; Gary L. Schieven; Katerina Leftheris

doi:10.1016/j.bmcl.2011.05.091

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors

Alaric J. Dyckman, Tianle Li, Sidney Pitt, Rosemary Zhang, Ding Ren Shen, Kim W. McIntyre, Kathleen M. Gillooly, David J. Shuster, Arthur M. Doweyko, John S. Sack, Kevin Kish, Susan E. Kiefer, John A. Newitt, Hongjian Zhang, Punit H. Marathe, Murray McKinnon, Joel C. Barrish, John H. Dodd, Gary L. Schieven, Katerina Leftheris

Chemistry

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

14 Scopus citations

Abstract

Pyrrolo[2,1-f][1,2,4]triazine based inhibitors of p38α have been prepared exploring functional group modifications at the C6 position. Incorporation of aryl and heteroaryl ketones at this position led to potent inhibitors with efficacy in in vivo models of acute and chronic inflammation.

Original language	English (US)
Pages (from-to)	4633-4637
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	15
DOIs	https://doi.org/10.1016/j.bmcl.2011.05.091
State	Published - Aug 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.2011.05.091

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Dyckman, A. J., Li, T., Pitt, S., Zhang, R., Shen, D. R., McIntyre, K. W., Gillooly, K. M., Shuster, D. J., Doweyko, A. M., Sack, J. S., Kish, K., Kiefer, S. E., Newitt, J. A., Zhang, H., Marathe, P. H., McKinnon, M., Barrish, J. C., Dodd, J. H., Schieven, G. L., & Leftheris, K. (2011). Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors. Bioorganic and Medicinal Chemistry Letters, 21(15), 4633-4637. https://doi.org/10.1016/j.bmcl.2011.05.091

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title = "Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors",

abstract = "Pyrrolo[2,1-f][1,2,4]triazine based inhibitors of p38α have been prepared exploring functional group modifications at the C6 position. Incorporation of aryl and heteroaryl ketones at this position led to potent inhibitors with efficacy in in vivo models of acute and chronic inflammation.",

author = "Dyckman, {Alaric J.} and Tianle Li and Sidney Pitt and Rosemary Zhang and Shen, {Ding Ren} and McIntyre, {Kim W.} and Gillooly, {Kathleen M.} and Shuster, {David J.} and Doweyko, {Arthur M.} and Sack, {John S.} and Kevin Kish and Kiefer, {Susan E.} and Newitt, {John A.} and Hongjian Zhang and Marathe, {Punit H.} and Murray McKinnon and Barrish, {Joel C.} and Dodd, {John H.} and Schieven, {Gary L.} and Katerina Leftheris",

year = "2011",

month = aug,

day = "1",

doi = "10.1016/j.bmcl.2011.05.091",

language = "English (US)",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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Dyckman, AJ, Li, T, Pitt, S, Zhang, R, Shen, DR, McIntyre, KW, Gillooly, KM, Shuster, DJ, Doweyko, AM, Sack, JS, Kish, K, Kiefer, SE, Newitt, JA, Zhang, H, Marathe, PH, McKinnon, M, Barrish, JC, Dodd, JH, Schieven, GL & Leftheris, K 2011, 'Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors', Bioorganic and Medicinal Chemistry Letters, vol. 21, no. 15, pp. 4633-4637. https://doi.org/10.1016/j.bmcl.2011.05.091

TY - JOUR

T1 - Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors

AU - Dyckman, Alaric J.

AU - Li, Tianle

AU - Pitt, Sidney

AU - Zhang, Rosemary

AU - Shen, Ding Ren

AU - McIntyre, Kim W.

AU - Gillooly, Kathleen M.

AU - Shuster, David J.

AU - Doweyko, Arthur M.

AU - Sack, John S.

AU - Kish, Kevin

AU - Kiefer, Susan E.

AU - Newitt, John A.

AU - Zhang, Hongjian

AU - Marathe, Punit H.

AU - McKinnon, Murray

AU - Barrish, Joel C.

AU - Dodd, John H.

AU - Schieven, Gary L.

AU - Leftheris, Katerina

PY - 2011/8/1

Y1 - 2011/8/1

N2 - Pyrrolo[2,1-f][1,2,4]triazine based inhibitors of p38α have been prepared exploring functional group modifications at the C6 position. Incorporation of aryl and heteroaryl ketones at this position led to potent inhibitors with efficacy in in vivo models of acute and chronic inflammation.

AB - Pyrrolo[2,1-f][1,2,4]triazine based inhibitors of p38α have been prepared exploring functional group modifications at the C6 position. Incorporation of aryl and heteroaryl ketones at this position led to potent inhibitors with efficacy in in vivo models of acute and chronic inflammation.

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ER -

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors

Abstract

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