Zobrazeno 1 - 10
of 50
pro vyhledávání: '"Kirrane, Thomas"'
Autor:
Raymond A. Kemper, Jennifer Burke, James V. Haist, Nelamangara Nagaraja, Charles A. Kennedy, Christian Eickmeier, Stephen J. Boyer, Stéphane De Lombaert, Xin Guo, John D. Huber, Alan David Swinamer, Jeffrey B. Madwed, Anne B. Eldrup, Kirrane Thomas M, Morris Karmazyn, Fariba Soleymanzadeh, Paul Kaplita, Eugene R. Hickey, Jörg Bentzien, Elizabeth Mainolfi
Publikováno v:
Journal of Medicinal Chemistry. 55:7114-7140
Sodium-hydrogen exchanger isoform 1 (NHE1) is a ubiquitously expressed transmembrane ion channel responsible for intracellular pH regulation. During myocardial ischemia, low pH activates NHE1 and causes increased intracellular calcium levels and aber
Autor:
Mohammed A. Kashem, Stanley Kugler, Lida Soleymanzadeh, Yunlong Zhang, Jeffery B. Madwed, Xin Guo, Kirrane Thomas M, Roger J. Snow, Alan David Swinamer, Jennifer Burke, Margaret M. O’Neill, Stephen J. Boyer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:738-742
A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were optimized for cellular potency and kinase selectivity. This led to the identification of c
Autor:
Zhaoming Xiong, Stephen J. Boyer, Lida Soleymanzadeh, Stanley Kugler, John Westbrook, Yunlong Zhang, Anil Kumar Padyana, Jennifer Burke, Jeffrey B. Madwed, Derek Cogan, Alan David Swinamer, Chris Sarko, Mohammed A. Kashem, Frank M. DiCapua, Kirrane Thomas M, Amy Gao, Roger J. Snow, Xin Guo, Margaret M. O’Neill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:733-737
A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were identified through high throughput screening. An RSK crystal structure and exploratory SAR
Autor:
Alison Kukulka, Ho Yin Lo, Roman Wolfgang Fleck, Raj Betageri, Mary Ann Hoermann, Usha R. Patel, Stéphane De Lombaert, Alisa K. Kabcenell, Richard H. Ingraham, Rajiv Sharma, Kirrane Thomas M, John R. Proudfoot, Neil A. Farrow, Chuk Chui Man
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6379-6383
A novel series of pyrazole sEH inhibitors is reported. Lead optimization efforts to replace the aniline core are also described. In particular, 2-pyridine, 3-pyridine and pyridazine analogs are potent sEH inhibitors with favorable CYP3A4 inhibitory a
Autor:
Tazmeen N. Fadra, Kirrane Thomas M, Carol A. Torcellini, Christopher Pargellis, Neil Moss, Jeffrey B. Madwed, Rachel R. Kroe, John R. Regan, Raj Betageri, Pier F. Cirillo, Eugene R. Hickey, Kevin Chungeng Qian, Richard M. Nelson, Steffen Breitfelder, Alan David Swinamer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4242-4247
Discovery of the pyrazole-naphthyl urea class of p38 MAP kinase inhibitors typified by the clinical candidate BIRB 796 has encouraged further exploration of this particular scaffold. Modification to the part of the inhibitor that occupies the adenine
Autor:
Donald Souza, Gerald Nabozny, Richard M. Nelson, Kirrane Thomas M, Lijiljana Zuvela-Jelaska, Daniel Kuzmich, Gilmore Thomas A, John R. Proudfoot, Renee Zindell, Josephine Pelletier, Abdelhakim Hammach, Jörg Bentzien, John R. Regan, David S. Thomson, Alison Kukulka, Younes Bekkali, Mark Stephen Ralph, Thomas Wai-Ho Lee
Publikováno v:
Journal of Medicinal Chemistry. 49:7887-7896
We report on the nuclear receptor binding affinities, cellular activities of transrepression and transactivation, and anti-inflammatory properties of a quinol-4-one and other A-ring mimetic containing nonsteroidal class of glucocorticoid agonists.
Autor:
Kirrane Thomas M, Xiao-Jun Wang, John R. Proudfoot, Jonathan Tan, Grozinger Karl G, Raj Betageri
Publikováno v:
Tetrahedron Letters. 41:5321-5324
3-Aryl-5-alkylpyrazoles undergo a highly regioselective arylation on N-1 atom with 4-fluoronitrobenzene in the presence of base to yield the corresponding 1-(4-nitrophenyl)pyrazoles.
Autor:
Jean Rancourt, Kirrane Thomas M, Rajiv Sharma, Martin Poirier, John R. Proudfoot, Susan Lukas, Montse Llinas-Brunet, Usha R. Patel, Dominik Wernic, Alisa K. Kabcenell, Pierre L. Beaulieu, Neil Moss, Scott Jakes, Vida Gorys, Jean Gauthier, Mario G. Cardozo, Liang Tong, Eugene R. Hickey, Dale R. Cameron, Jean-Marie Ferland, Raj Betageri, Richard H. Ingraham, James Gillard, Ghiro Elise
Publikováno v:
Journal of Medicinal Chemistry. 42:1757-1766
p56lck is a member of the src family of tyrosine kinases. Through modular binding units called SH2 domains, p56lck promotes phosphotyrosine-dependent protein-protein interactions and plays a critical role in signal transduction events that lead to T-
Autor:
Boyer, Stephen J., Burke, Jennifer, Guo, Xin, Kirrane, Thomas M., Snow, Roger J., Zhang, Yunlong, Sarko, Chris, Soleymanzadeh, Lida, Swinamer, Alan, Westbrook, John, DiCapua, Frank, Padyana, Anil, Cogan, Derek, Gao, Amy, Xiong, Zhaoming, Madwed, Jeffrey B., Kashem, Mohammed, Kugler, Stanley, O’Neill, Margaret M.
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 1 January 2012 22(1):733-737
Autor:
Kirrane, Thomas M., Boyer, Stephen J., Burke, Jennifer, Guo, Xin, Snow, Roger J., Soleymanzadeh, Lida, Swinamer, Alan, Zhang, Yunlong, Madwed, Jeffery B., Kashem, Mohammed, Kugler, Stanley, O’Neill, Margaret M.
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 1 January 2012 22(1):738-742