Výsledky vyhledávání - "Bradley Henkle"

Identification of triazolopyridazinones as potent p38α inhibitors

Autor: Claire L. M. Jackson, Bradley Henkle, Matthew R. Lee, Brad Herberich, Andrew Tasker, Samer Chmait, Qiurong Liu, Christiaan J. M. Saris, Faye Hsieh, Liping H. Pettus, Christopher Mohr, Lisa Sherman, Ryan Wurz, Lu Min Wong

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:1226-1229

Structure-activity relationship (SAR) investigations of a novel class of triazolopyridazinone p38α mitogen activated protein kinase (MAPK) inhibitors are disclosed. From these studies, increased in vitro potency was observed for 2,6-disubstituted ph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9647181f2f2fd256c513ab351fdba20b
https://doi.org/10.1016/j.bmcl.2011.11.067

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3-Amino-7-phthalazinylbenzoisoxazoles as a Novel Class of Potent, Selective, and Orally Available Inhibitors of p38α Mitogen-Activated Protein Kinase

Publikováno v: Journal of Medicinal Chemistry. 51:6280-6292

The p38 mitogen-activated protein kinase (MAPK) is a central signaling molecule in many proinflammatory pathways, regulating the cellular response to a multitude of external stimuli including heat, ultraviolet radiation, osmotic shock, and a variety

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7087b9c4f5722d23b003b38ab86133ff
https://doi.org/10.1021/jm8005405

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Discovery of pyridazinopyridinones as potent and selective p38 mitogen-activated protein kinase inhibitors

Autor: Faye Hsieh, Elizabeth M. Doherty, Bradley Henkle, Helen J. McBride, Lisa Sherman, Lu Min Wong, Andrew Tasker, Matthew R. Lee, Christiaan J. M. Saris, Matthew H. Plant, Bin Wu, Liping H. Pettus, Hui-Ling Wang, Ryan Wurz

Publikováno v: Journal of medicinal chemistry. 53(17)

The p38 mitogen-activated protein kinase (MAPK) plays an important role in the production of proinflammatory cytokines, making it an attractive target for the treatment of various inflammatory diseases. A series of pyridazinopyridinone compounds were

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4efcedb28e563a4aaad90be4ae67924d
https://pubmed.ncbi.nlm.nih.gov/20712346

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Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase

Autor: Liping H, Pettus, Ryan P, Wurz, Shimin, Xu, Brad, Herberich, Bradley, Henkle, Qiurong, Liu, Helen J, McBride, Sharon, Mu, Matthew H, Plant, Christiaan J M, Saris, Lisa, Sherman, Lu Min, Wong, Samer, Chmait, Matthew R, Lee, Christopher, Mohr, Faye, Hsieh, Andrew S, Tasker

Publikováno v: Journal of medicinal chemistry. 53(7)

The p38alpha mitogen-activated protein (MAP) kinase is a central signaling molecule in many proinflammatory pathways, regulating the cellular response to a multitude of external stimuli including heat, ultraviolet radiation, osmotic shock, and a vari

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::70a8588035612689d1c02ad6415d9e18
https://pubmed.ncbi.nlm.nih.gov/20218619

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Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase

Autor: Ryan P. Wurz, Liping H. Pettus, Bradley Henkle, Lisa Sherman, Matthew Plant, Kent Miner, Helen J. McBride, Lu Min Wong, Christiaan J.M. Saris, Matthew R. Lee, Samer Chmait, Christopher Mohr, Faye Hsieh, Andrew S. Tasker

Publikováno v: Bioorganicmedicinal chemistry letters. 20(5)

A novel class of pyrazolopyridazine p38alpha mitogen-activated protein kinase (MAPK) inhibitors is disclosed. A structure activity relationship (SAR) investigation was conducted driven by the ability of these compounds to inhibit the p38alpha enzyme,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2906e3074f6867c308cf5e4c2b1a9be
https://pubmed.ncbi.nlm.nih.gov/20138761

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Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase

Autor: Samer Chmait, Lu Min Wong, Faye Hsieh, Liping H. Pettus, Ryan Wurz, Andrew Tasker, Lisa Sherman, Matthew R. Lee, Kent Miner, Helen J. McBride, Matthew H. Plant, Shimin Xu, Christiaan J. M. Saris, Christopher Mohr, Bradley Henkle

Publikováno v: Bioorganicmedicinal chemistry letters. 19(16)

A novel class of pyrazolopyridazine p38α mitogen-activated protein kinase (MAPK) inhibitors is disclosed. A structure activity relationship (SAR) investigation was conducted driven by the ability of these compounds to inhibit the p38α enzyme, the s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dd51e2be792e935e554fc47693b7163f
https://pubmed.ncbi.nlm.nih.gov/19574047

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Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold

Publikováno v: Journal of medicinal chemistry. 51(20)

Investigations into the structure-activity relationships (SAR) of a series of phthalazine-based inhibitors of p38 are described. These efforts originated from quinazoline 1 and through rational design led to the development of a series of orally bioa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4472ff7afe3b7f856819b7fe8180af1c
https://pubmed.ncbi.nlm.nih.gov/18817365

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Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase

Autor: Lillian Liao, Bradley Henkle, Violeta Yu, Rashid Syed, Graham Richard Jang, Timothy S. Harvey, Randall W. Hungate, Yanyan Tudor, Celia Dominguez, Lu Min Wong, Nuria A. Tamayo, Scot Middleton, David Powers, Martin H. Goldberg

Publikováno v: Bioorganicmedicinal chemistry letters. 15(9)

Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c7beff53dd4a69f2db09421329f14f61
https://pubmed.ncbi.nlm.nih.gov/15837335

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