Design and Synthesis of Potent, Selective, and Orally Bioavailable Tetrasubstituted Imidazole Inhibitors of p38 Mitogen-Activated Protein Kinase

Nigel J. Liverton; John W. Butcher; Christopher F. Claiborne; David A. Claremon; Brian E. Libby; Kevin T. Nguyen; Steven M. Pitzenberger; Harold G. Selnick; Garry R. Smith; Andrew Tebben; Joseph P. Vacca; Sandor L. Varga; Lily Agarwal; Kim Dancheck; Amy J. Forsyth; Daniel S. Fletcher; Betsy Frantz; William A. Hanlon; Coral F. Harper; Scott J. Hofsess; Matthew Kostura; Jiunn Lin; Sylvie Luell; Edward A. O'Neill; Chad J. Orevillo; Margaret Pang; Janey Parsons; Anna Rolando; Yousif Sahly; Denise M. Visco; Stephen J. O'Keefe

doi:10.1021/jm9805236

Design and Synthesis of Potent, Selective, and Orally Bioavailable Tetrasubstituted Imidazole Inhibitors of p38 Mitogen-Activated Protein Kinase

Journal of Medicinal Chemistry ◽

10.1021/jm9805236 ◽

1999 ◽

Vol 42 (12) ◽

pp. 2180-2190 ◽

Cited By ~ 148

Author(s):

Nigel J. Liverton ◽

John W. Butcher ◽

Christopher F. Claiborne ◽

David A. Claremon ◽

Brian E. Libby ◽

...

Keyword(s):

Protein Kinase ◽

Mitogen Activated Protein Kinase ◽

Design And Synthesis ◽

Mitogen Activated Protein ◽

Orally Bioavailable

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ChemInform Abstract: Design and Synthesis of Potent, Selective, and Orally Bioavailable Tetrasubstituted Imidazole Inhibitors of p38 Mitogen-Activated Protein Kinase.

ChemInform ◽

10.1002/chin.199939120 ◽

2010 ◽

Vol 30 (39) ◽

pp. no-no

Author(s):

Nigel J. Liverton ◽

et al. et al.

Keyword(s):

Protein Kinase ◽

Mitogen Activated Protein Kinase ◽

Design And Synthesis ◽

Mitogen Activated Protein ◽

Orally Bioavailable

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Discovery of 6-(2,4-Difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (Pamapimod) and 6-(2,4-Difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as Orally Bioavailable and Highly Selective Inhibitors of p38α Mitogen-Activated Protein Kinase

Journal of Medicinal Chemistry ◽

10.1021/jm101423y ◽

2011 ◽

Vol 54 (7) ◽

pp. 2255-2265 ◽

Cited By ~ 29

Author(s):

David M. Goldstein ◽

Michael Soth ◽

Tobias Gabriel ◽

Nolan Dewdney ◽

Andreas Kuglstatter ◽

...

Keyword(s):

Protein Kinase ◽

Mitogen Activated Protein Kinase ◽

Selective Inhibitors ◽

Mitogen Activated Protein ◽

Orally Bioavailable

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Design and Synthesis of Highly Selective Brain Penetrant p38α Mitogen-Activated Protein Kinase Inhibitors

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.0c01773 ◽

2021 ◽

Author(s):

Niklas M. Tormählen ◽

Mariella Martorelli ◽

Annette Kuhn ◽

Florian Maier ◽

Jamil Guezguez ◽

...

Keyword(s):

Protein Kinase ◽

Kinase Inhibitors ◽

Protein Kinase Inhibitors ◽

Mitogen Activated Protein Kinase ◽

Design And Synthesis ◽

Mitogen Activated Protein

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Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - a promising target for liver regeneration

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2021.113371 ◽

2021 ◽

pp. 113371

Author(s):

Bent Pfaffenrot ◽

Philip Klövekorn ◽

Michael Juchum ◽

Roland Selig ◽

Wolfgang Albrecht ◽

...

Keyword(s):

Protein Kinase ◽

Liver Regeneration ◽

Mitogen Activated Protein Kinase ◽

Design And Synthesis ◽

Promising Target ◽

Mitogen Activated Protein ◽

Protein Kinase Kinase

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1333: Proteinase-Activated Receptor-2 Activation of the Mitogen Activated Protein Kinase Pathway in Human Cultured Prostate Stromal Cells

The Journal of Urology ◽

10.1016/s0022-5347(18)38558-6 ◽

2004 ◽

Vol 171 (4S) ◽

pp. 351-351

Author(s):

Andrew Myatt ◽

Duncan R. Harriss ◽

Stephen J. Hill

Keyword(s):

Protein Kinase ◽

Stromal Cells ◽

Mitogen Activated Protein Kinase ◽

Mitogen Activated Protein ◽

Kinase Pathway

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Auto-induction of Transforming Growth Factor-βl (TGF-β1) mRNA in porcine granulosa cells and inhibition by a Mitogen-Activated Protein Kinase (MAPK) kinase inhibitor

Journal of the Society for Gynecologic Investigation ◽

10.1016/s1071-5576(97)86103-5 ◽

1998 ◽

Vol 5 (1) ◽

pp. 45A-45A

Author(s):

Y MAU ◽

H FONG ◽

J DAVIS ◽

J MAY

Keyword(s):

Growth Factor ◽

Protein Kinase ◽

Granulosa Cells ◽

Transforming Growth Factor ◽

Kinase Inhibitor ◽

Mitogen Activated Protein Kinase ◽

Mapk Kinase ◽

Porcine Granulosa Cells ◽

Mitogen Activated Protein ◽

Tgf Β1

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Down-regulation of the mitogen-activated protein kinase cascade immediately before parturition in the rat myometrium

Journal of the Society for Gynecologic Investigation ◽

10.1016/s1071-5576(98)00030-6 ◽

1998 ◽

Vol 5 (6) ◽

pp. 304-310 ◽

Cited By ~ 4

Author(s):

A Ruzycky

Keyword(s):

Protein Kinase ◽

Mitogen Activated Protein Kinase ◽

Down Regulation ◽

Mitogen Activated Protein ◽

Kinase Cascade ◽

Protein Kinase Cascade

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876 Human urotensin II activates the sarcolemmal Na+/H+ exchanger: roles of protein kinase C and mitogen-activated protein kinase(s)

European Journal of Heart Failure Supplements ◽

10.1016/s1567-4215(03)90561-3 ◽

2003 ◽

Vol 2 (1) ◽

pp. 186

Author(s):

K KATO ◽

M YASUTAKE ◽

D JIA ◽

Y KUSAMA ◽

T TAKANO

Keyword(s):

Protein Kinase C ◽

Protein Kinase ◽

Mitogen Activated Protein Kinase ◽

Urotensin Ii ◽

Kinase C ◽

Mitogen Activated Protein

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Age-Related Changes in Activation of Mitogen-Activated Protein Kinase Cascades by Oxidative Stress

Journal of Investigative Dermatology ◽

10.1038/jidsp.1998.7 ◽

1998 ◽

Vol 3 (1) ◽

pp. 23-27 ◽

Cited By ~ 9

Author(s):

Kathryn Z Guyton ◽

Myriani Gorospe ◽

Xiantao Wang ◽

Yolanda D Mock ◽

Gertrude C Kokkonen ◽

...

Keyword(s):

Oxidative Stress ◽

Protein Kinase ◽

Mitogen Activated Protein Kinase ◽

Age Related ◽

Mitogen Activated Protein ◽

Age Related Changes

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P2888 p38 mitogen-activated protein kinase-mediated fibrosis following myocardial infarction is regulated by connective tissue growth factor

European Heart Journal ◽

10.1016/s0195-668x(03)95666-1 ◽

2003 ◽

Vol 24 (5) ◽

pp. 554 ◽

Cited By ~ 1

Author(s):

F SEE

Keyword(s):

Myocardial Infarction ◽

Growth Factor ◽

Protein Kinase ◽

Connective Tissue ◽

Connective Tissue Growth Factor ◽

Tissue Growth ◽

Mitogen Activated Protein Kinase ◽

Mitogen Activated Protein

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