Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Gillian Greig"'
Autor:
Bruno Roy, Claudio Sturino, Nicolas Lachance, Robert Zamboni, Kathleen M. Metters, Christine Brideau, Lianhai Li, John Scheigetz, Danielle Denis, Deborah Slipetz, Marie-Claude Carrière, Elizabeth Cauchon, Gillian Greig, Gary P. O'Neill, Carl Berthelette, Michael J. Boyd, Marie-Claude Mathieu, Sonia Lamontagne, Nicole Sawyer, Robert N. Young, Nancy N. Tsou, Zhaoyin Wang, Stacia Kargman, Marc Labelle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3043-3048
A novel indole series of PGD2 receptor (DP receptor) antagonists is presented. Optimization of this series led to the identification of potent and selective DP receptor antagonists. In particular, antagonists 35 and 36 were identified with Ki values
Autor:
Gary P. O'Neill, A. Daniel Malebranche, Jean-Pierre Morello, Gillian Greig, François G. Gervais, Danielle Denis, Nicole Sawyer, Christian Beaulieu
Publikováno v:
Molecular Pharmacology. 67:1834-1839
The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTH2) is a G protein-coupled receptor whose function in vivo has been incompletely characterized. One of the reasons is that its current known ligands, prostaglandi
Autor:
Richard Friesen, Gillian Greig, Nicole Sawyer, Bernard Cote, Stacia Kargman, Sonia Lamontagne, Kathleen M. Metters, Richard Frenette, Yves Ducharme, Gary P. O'Neill, François Nantel, Marie-Claude Carrière, Evelyn Martins, Anne Chateauneuf, Danielle Denis, Marc Blouin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1155-1160
The synthesis and the EP(1) receptor binding affinity of 2,3-diarylthiophene derivatives are described. The evaluation of the structure-activity relationship (SAR) in this series led to the identification of compounds 4, 7, and 12a, which exhibit hig
Autor:
Gillian Greig, Deborah Slipetz, Gary P. O'Neill, Sonia Lamontagne, Jennifer Wang, Christian Beaulieu, Zhaoyin Wang, Danielle Denis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:3195-3199
A series of 2-substituted N-benzyl benzimidazole containing molecules has been synthesized and its structure-activity relationship for the human DP receptor has been evaluated. Selective DP antagonists with nanomolar potency for the DP receptor were
Autor:
Denis Riendeau, Stella Charleson, Jocelyne Guay, Elizabeth Wong, Denise M. Visco, Robert Gordon, Lijing Xu, Michel Therien, Gillian Greig, Petpiboon Prasit, Chi-Chung Chan, W. Cameron Black, Jacques Yves Gauthier, David Claveau, Erich L. Grimm, Wanda Cromlish, Christine Brideau, Cheuk K. Lau, Chun-Sing Li
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:3181-3186
By inserting an oxygen link between the 3-fluorophenyl and the lactone ring of 5,5-dimethyl-3-(3fluorophenyl)-4-(4-methanesulfonylphenyl)-2 (5H)-furanone 1 (DFU), analogs with enhanced in vitro COX-2 inhibitory potency as well as in vivo potency in m
Autor:
P. Jolicoeur, P. Prasit, R. Gordon, Christine Brideau, Stella Charleson, Denis Riendeau, Deborah A. Nicoll-Griffith, Gillian Greig, Denise M. Visco, Diane Ethier, C. Chan, Nathalie Ouimet, Yves Leblanc, Zhaoyin Wang, Greg Hughes, Lijing Xu, W. C. Black, Jocelyne Guay, David Claveau, Nathalie Chauret
Publikováno v:
Journal of Medicinal Chemistry. 42:1274-1281
Cyclopentenones containing a 4-(methylsulfonyl)phenyl group in the 3-position and a phenyl ring in the 2-position are selective inhibitors of cyclooxygenase-2 (COX-2). The selectivity for COX-2 over COX-1 is dramatically improved by substituting the
Autor:
Li Jing Xu, Denise M. Visco, Diane Ethier, Gillian Greig, Denis Riendeau, Jacques Yves Gauthier, Stella Charleson, Chi-Chung Chan, Robert Gordon, Denis Deschenes, Yves Girard, Richard Friesen, Robert N. Young, Elizabeth Wong, Christine Brideau, Chantal Savoie, Daniel Dube, Zhaoyin Wang, Rejean Fortin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:2777-2782
A series of novel 2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines has been synthesized and evaluated with respect to their ability to inhibit the isozymes of cyclooxygenase, COX-1, and COX-2. Optimum COX-2 activity is observed by introduction of a su
Autor:
Robert Zamboni, Jocelyne Guay, Stella Charleson, M.D. Percival, Jean-Pierre Falgueyret, Joseph A. Mancini, Susan Boyce, Michael J. Therien, Lijing Xu, R. Gordon, Stacia Kargman, Anthony W. Ford-Hutchinson, Gillian Greig, Marc Ouellet, Denis Riendeau, Petpiboon Prasit, Serge Leger, Zhaoyin Wang, J.K. Webb, Diane Ethier, Chi-Chung Chan, Gary P. O'Neill, Robert N. Young, Ian W. Rodger, Wanda Cromlish, Christine Brideau, Jillian F. Evans, Michael J. Gresser, E. Wong
Publikováno v:
British Journal of Pharmacology. 121:105-117
1. DFU (5,5-dimethyl-3-(3-fluorophenyl)-4-(4-methylsulphonyl)phenyl-2(5H)-furan one) was identified as a novel orally active and highly selective cyclo-oxygenase-2 (COX-2) inhibitor. 2. In CHO cells stably transfected with human COX isozymes, DFU inh
Autor:
Gillian Greig, Michael J. Therien, Wanda Cromlish, C. C. Chan, Christine Brideau, Robert Gordon, Patrick Roy, Chun-Sing Li, Stacia Kargman, Zhaoyin Wang, Denis Riendeau, Cheuk K. Lau, Yves Leblanc, Li Jing Xu, Gary P. O'Neill, P. Prasit, Jacques Yves Gauthier
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:47-52
A series of 5,6-diarylimidazo[2.1-b]thiazole compounds were prepared and their inhibitory potencies against COX-2 and Cox-1 enzymes were measured. This led to the identification of L-766,112 as a potent, orally active and selective inhibitor of the C
Autor:
Michael J. Therien, Li Jing Xu, Robert Gordon, C. C. Chan, Diane Ethier, Elizabeth Wong, Gillian Greig, Jocelyne Guay, Wanda Cromlish, Christine Brideau, Cheuk K. Lau, C. van Staden, Jacques Yves Gauthier, Yves Leblanc, Gary P. O'Neill, P. Prasit, Nathalie Chauret, Stacia Kargman, José M. Silva, Patrick Roy, Richard G. Ball
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:57-62
A series of 5,6-diarylthiazolo[3,2-b][1,2,4]triazoles was prepared for evaluation of potency and selectivity against human COX-1 and COX-2 enzymes. This lead to the discovery of L-768,277, a potent and selective COX-2 inhibitor that also demonstrated