-
1
-
-
0028605318
-
A protein kinase involved in the regulation of inflammatory cytokine biosynthesis
-
Lee, J. C.; Laydon, J. T.; McDonell, P. S.; Gallagher, T. F.; Kumar, S.; Green, D.; McNulty, D.; Blumenthal, M. J.; Heys, J. R.; Landvatter, S. W.; Strickler, J. E.; McLaughlin, M. M.; Siemens, I. R.; Fisher, S. M.; Livi, G. P.; White, J. R.; Adams, J. L.; Young, P. R. A protein kinase involved in the regulation of inflammatory cytokine biosynthesis. Nature 1994, 372, 739.
-
(1994)
Nature
, vol.372
, pp. 739
-
-
Lee, J.C.1
Laydon, J.T.2
McDonell, P.S.3
Gallagher, T.F.4
Kumar, S.5
Green, D.6
McNulty, D.7
Blumenthal, M.J.8
Heys, J.R.9
Landvatter, S.W.10
Strickler, J.E.11
McLaughlin, M.M.12
Siemens, I.R.13
Fisher, S.M.14
Livi, G.P.15
White, J.R.16
Adams, J.L.17
Young, P.R.18
-
2
-
-
0027936755
-
A MAP Kinase targetted by endotoxin and hyperosmolarity in mammalian cells
-
Han, J.; Lee, J. -D.; Bibbs, L.; Ulevitch, R. J. A MAP Kinase targetted by endotoxin and hyperosmolarity in mammalian cells Science 1994, 265, 808.
-
(1994)
Science
, vol.265
, pp. 808
-
-
Han, J.1
Lee, J.-D.2
Bibbs, L.3
Ulevitch, R.J.4
-
3
-
-
0028022750
-
A novel kinase cascade triggered by stress and heat shock that stimulates MAPKAP kinase-2 and phosphorylation of the small heat shock protein
-
Rouse, J.; Cohen, P.; Trigon, S.; Morange, M.; Alonso-Llamazares, A.; Zamanillo, D.; Hunt, T.; Nebreda, A. R. A novel kinase cascade triggered by stress and heat shock that stimulates MAPKAP kinase-2 and phosphorylation of the small heat shock protein Cell 1994, 78, 1027.
-
(1994)
Cell
, vol.78
, pp. 1027
-
-
Rouse, J.1
Cohen, P.2
Trigon, S.3
Morange, M.4
Alonso-Llamazares, A.5
Zamanillo, D.6
Hunt, T.7
Nebreda, A.R.8
-
4
-
-
0027761036
-
-
Lee, J. C.; Badger, A. M.; Griswald, D. E.; Dunnington, D.; Truenh, A.; Votta, B.; White, J. R.; Young, P. R.; Bender, P. E. Annals New York Academy of Sciences 1993, 896, 149.
-
(1993)
Annals New York Academy of Sciences
, vol.896
, pp. 149
-
-
Lee, J.C.1
Badger, A.M.2
Griswald, D.E.3
Dunnington, D.4
Truenh, A.5
Votta, B.6
White, J.R.7
Young, P.R.8
Bender, P.E.9
-
5
-
-
0030426902
-
Pharmacological profile of SB 203580, a selective inhibitor of cytokine supppresive binding protein / p38 kinase in animal models of arthritis, bone resorption, endotoxin shock and immune function
-
a)
-
a) Badger, A. M.; Bradbeer, J. N.; Votta, B.; Lee, J. C.; Adams, J. L.; Griswold, D. E. Pharmacological profile of SB 203580, a selective inhibitor of cytokine supppresive binding protein / p38 kinase in animal models of arthritis, bone resorption, endotoxin shock and immune function. J Pharmacol. Exp. Ther. 1996, 279, 1453.
-
(1996)
J. Pharmacol. Exp. Ther.
, vol.279
, pp. 1453
-
-
Badger, A.M.1
Bradbeer, J.N.2
Votta, B.3
Lee, J.C.4
Adams, J.L.5
Griswold, D.E.6
-
6
-
-
10144243335
-
1-Substituted 4-Aryl-5-pyridinylimidazoles: A New Class of Cytokine Suppressive Drugs with Low 5-Lipoxygenase and Cyclooxygenase Inhibitory Potency
-
b)
-
b) Boehm, J. C.; Smietana, J. M.; Sorensen, M. E.; Garigipatti, R. S.; Gallagher, T. F.; Sheldrake, P. L.; Bradbeer, J.; Badger, A. M.; Laydon, J. T.; Lee, J. C.; Hillegass, L. M.; Griswold, D. E.; Breton, J. J.; Chabot-Fletcher, M. C.; Adams, J. L. 1-Substituted 4-Aryl-5-pyridinylimidazoles: A New Class of Cytokine Suppressive Drugs with Low 5-Lipoxygenase and Cyclooxygenase Inhibitory Potency. J. Med. Chem. 1996, 39, 3929.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 3929
-
-
Boehm, J.C.1
Smietana, J.M.2
Sorensen, M.E.3
Garigipatti, R.S.4
Gallagher, T.F.5
Sheldrake, P.L.6
Bradbeer, J.7
Badger, A.M.8
Laydon, J.T.9
Lee, J.C.10
Hillegass, L.M.11
Griswold, D.E.12
Breton, J.J.13
Chabot-Fletcher, M.C.14
Adams, J.L.15
-
7
-
-
0032491233
-
Pyrroles and other heterocycles as inhibitors of p38 kinase
-
De Laszlo, S. E.; Visco, D.; Agarwal, L.; Chang, L.; Chin, J.; Croft, G.; Forsyth, A.; Fletcher, D.; Frantz, B.; Hacker, C.; Hanlon, W.; Harper, C.; Kostura, M.; Li, B.; Luell, S.; MacCoss, M.; Mantlo, N.; O'Neill, E. A.; Orevillo, C.; Pang, M.; Parsons, J.; Rolando, A.; Sahly, Y.; Sidler, K.; Widmer, R. W.; O'Keefe, S. J. Pyrroles and other heterocycles as inhibitors of p38 kinase. Bioorg. Med. Chem. Lett. 1998, 8, 2689.
-
(1998)
Bioorg. Med. Chem. Lett.
, vol.8
, pp. 2689
-
-
De Laszlo, S.E.1
Visco, D.2
Agarwal, L.3
Chang, L.4
Chin, J.5
Croft, G.6
Forsyth, A.7
Fletcher, D.8
Frantz, B.9
Hacker, C.10
Hanlon, W.11
Harper, C.12
Kostura, M.13
Li, B.14
Luell, S.15
MacCoss, M.16
Mantlo, N.17
O'Neill, E.A.18
Orevillo, C.19
Pang, M.20
Parsons, J.21
Rolando, A.22
Sahly, Y.23
Sidler, K.24
Widmer, R.W.25
O'Keefe, S.J.26
more..
-
8
-
-
0033578080
-
Design and synthesis of potent, selective and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen activated protein kinase
-
a)
-
a) Liverton, N. J.; Butcher, J. W.; Claiborne, C. F.; Claremon, D. A.; Libby, B. E.; Ngyuen, K. T.; Pitzenberger, S. M.; Selnick, H. G.; Smith, G. R.; Tebben, A.; Vacca, J. P.; Varga, S. L.; Agarwal, L.; Danheck, K.; Forsyth, A. J.; Fletcher, D. S.; Frantz, B.; Hanlon, W. A.; Harper, C. F.; Hofsess, S. J.; Kostura, M.; Lin, J.; Luell, S.; O'Neil, E. A.; Orevillo, C. J.; Pang, M.; Parsons, J.; Rolondo, A.; Sahly, Y.; Visco, D. M.; O'Keefe, S. J. Design and synthesis of potent, selective and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen activated protein kinase. J. Med. Chem. 1999, 42, 2180.
-
(1999)
J. Med. Chem.
, vol.42
, pp. 2180
-
-
Liverton, N.J.1
Butcher, J.W.2
Claiborne, C.F.3
Claremon, D.A.4
Libby, B.E.5
Ngyuen, K.T.6
Pitzenberger, S.M.7
Selnick, H.G.8
Smith, G.R.9
Tebben, A.10
Vacca, J.P.11
Varga, S.L.12
Agarwal, L.13
Danheck, K.14
Forsyth, A.J.15
Fletcher, D.S.16
Frantz, B.17
Hanlon, W.A.18
Harper, C.F.19
Hofsess, S.J.20
Kostura, M.21
Lin, J.22
Luell, S.23
O'Neil, E.A.24
Orevillo, C.J.25
Pang, M.26
Parsons, J.27
Rolondo, A.28
Sahly, Y.29
Visco, D.M.30
O'Keefe, S.J.31
more..
-
11
-
-
27744595780
-
-
Intl. Patent WO 03000682
-
Biftu, T.; Colletti, S. L.; McIntyre, C. J.; Schmatz, D. M.; Feng, D. D.; Doherty, J. B.; Liang, G. -B.; Liverton, N. J.; Beresis, R.; Berger, R.; Claremon, D. A.; Kovacs, E. W.; Qian, X. Intl. Patent, 2003, WO 03000682.
-
(2003)
-
-
Biftu, T.1
Colletti, S.L.2
McIntyre, C.J.3
Schmatz, D.M.4
Feng, D.D.5
Doherty, J.B.6
Liang, G.-B.7
Liverton, N.J.8
Beresis, R.9
Berger, R.10
Claremon, D.A.11
Kovacs, E.W.12
Qian, X.13
-
12
-
-
27744509288
-
-
a) Intl. Patent WO 98/27098
-
a) Bemis, G. W.; Salituro, F. G.; Duffy, J. P.; Cochran, J. E.; Harrington, E. M.; Murcko, M. A.; Wilson, K. P.; Su, M.; Galullo, V. P. Intl. Patent, 1998, WO 98/27098.
-
(1998)
-
-
Bemis, G.W.1
Salituro, F.G.2
Duffy, J.P.3
Cochran, J.E.4
Harrington, E.M.5
Murcko, M.A.6
Wilson, K.P.7
Su, M.8
Galullo, V.P.9
-
14
-
-
27744493240
-
-
US Patent 147,080
-
Bemis, G. W.; Salituro, F. G.; Duffy, J. P.; Harrington, E. M. US Patent, 2000, 6, 147,080.
-
(2000)
, vol.6
-
-
Bemis, G.W.1
Salituro, F.G.2
Duffy, J.P.3
Harrington, E.M.4
-
15
-
-
27744486277
-
-
27th National Medicinal Chemistry Symposium Kansas City, MO, June 13-17
-
Salituro, F. G. 27th National Medicinal Chemistry Symposium, Kansas City, MO, June 13-17, 2000.
-
(2000)
-
-
Salituro, F.G.1
-
16
-
-
27744530485
-
-
note
-
Resonance structure of VX-745 (26) and its reduced con-gener 24; the aromatic resonance form is thought to contribute substantially to observed properties of these molecules.
-
-
-
-
17
-
-
17344381323
-
p38 MAP kinase inhibitors. Part 1: Design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold
-
Natarajan, S. R.; Wisnoski, D. D.; Singh, S. B.; Stelmach, J. E.; O'Neill, E. A.; Schwartz, C. D.; Thompson, C. M.; Fitzgerald, C. E.; O'keefe, S. J.; Kumar, S.; Hop, C. E. C. A.; Zaller, D. M.; Schmatz, D. M.; Doherty, J. B. p38 MAP kinase inhibitors. Part 1: Design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold. Bioorg. Med. Chem. Lett. 2003, 13, 273.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 273
-
-
Natarajan, S.R.1
Wisnoski, D.D.2
Singh, S.B.3
Stelmach, J.E.4
O'Neill, E.A.5
Schwartz, C.D.6
Thompson, C.M.7
Fitzgerald, C.E.8
O'Keefe, S.J.9
Kumar, S.10
Hop, C.E.C.A.11
Zaller, D.M.12
Schmatz, D.M.13
Doherty, J.B.14
-
18
-
-
12644277392
-
The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase
-
Wilson, K. P.; McCaffrey, P. G.; Hsiao, K.; Pazhanisamy, P.; Galullo, V.; Bemis, G. W.; Fitzgibbon, M. J.; Caron, P. R.; Murcko, M. A.; So, M. S. S. The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase. Chem. Biol. 1997, 4, 423.
-
(1997)
Chem. Biol.
, vol.4
, pp. 423
-
-
Wilson, K.P.1
McCaffrey, P.G.2
Hsiao, K.3
Pazhanisamy, P.4
Galullo, V.5
Bemis, G.W.6
Fitzgibbon, M.J.7
Caron, P.R.8
Murcko, M.A.9
So, M.S.S.10
-
19
-
-
0032530336
-
Structural basis of inhibitor selectivity in MAP Kinases
-
Wang, Z.; Canagarajah, B. J.; Boehm, J. C.; Kassisa, S.; Cobb, M. H.; Young, P. R.; Abdel-Meguid, S.; Adams, J. L.; Goldsmith, E. J. Structural basis of inhibitor selectivity in MAP Kinases. Structure 1998, 6, 1117.
-
(1998)
Structure
, vol.6
, pp. 1117
-
-
Wang, Z.1
Canagarajah, B.J.2
Boehm, J.C.3
Kassisa, S.4
Cobb, M.H.5
Young, P.R.6
Abdel-Meguid, S.7
Adams, J.L.8
Goldsmith, E.J.9
-
20
-
-
27744461923
-
-
Unpublished Results 2005. Partial Charges and dipole moments were derived from the geometry optimization of each scaffold (represented by 25 and 27) with the Hartree-Fock method using 6-31G** basis set
-
Nam, K.; Natarajan, S. R.; Doherty, J. B. Unpublished Results 2005. Partial Charges and dipole moments were derived from the geometry optimization of each scaffold (represented by 25 and 27) with the Hartree-Fock method using 6-31G** basis set.
-
-
-
Nam, K.1
Natarajan, S.R.2
Doherty, J.B.3
-
21
-
-
0041318841
-
Structural basis for p38α MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity
-
Fitzgerald, C. E.; Patel, S. B.; Becker, J. W.; Cameron, P. M.; Zaller, D.; Pikounis, V. B.; O'Keefe, S. J.; Scapin, G. Structural basis for p38α MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity. Nat. Str. Biol. 2003, 10, 764.
-
(2003)
Nat. Str. Biol.
, vol.10
, pp. 764
-
-
Fitzgerald, C.E.1
Patel, S.B.2
Becker, J.W.3
Cameron, P.M.4
Zaller, D.5
Pikounis, V.B.6
O'Keefe, S.J.7
Scapin, G.8
-
22
-
-
10744219935
-
SAR of 3,4-Dihydro[3,2-d]pyrimidone p38 inhibitors
-
Liu, L.; Stelmach, J. E.; Natarajan, S. R.; Chen, M. -H.; Singh, S. B.; Schwartz, C. D.; Fitzgerald, C. E.; O'Keefe, S. J.; Zaller, D. M.; Schmatz, D. M.; Doherty, J. B. SAR of 3,4-Dihydro[3,2-d]pyrimidone p38 inhibitors. Bioorg. Med. Chem. Lett. 2003, 13, 3979.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 3979
-
-
Liu, L.1
Stelmach, J.E.2
Natarajan, S.R.3
Chen, M.-H.4
Singh, S.B.5
Schwartz, C.D.6
Fitzgerald, C.E.7
O'Keefe, S.J.8
Zaller, D.M.9
Schmatz, D.M.10
Doherty, J.B.11
-
23
-
-
27744460974
-
-
Unpublished results
-
Natarajan, S. R.; Wisnoski, D. W.; O'Keefe, S. J.; Zaller, D. M.; Doherty, J. B. Unpublished results, 2002.
-
(2002)
-
-
Natarajan, S.R.1
Wisnoski, D.W.2
O'Keefe, S.J.3
Zaller, D.M.4
Doherty, J.B.5
-
24
-
-
18744397820
-
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP Kinase
-
Stelmach, J. E.; Liu, L.; Patel, S. B.; Pivnichny, J. V.; Scapin, G.; Singh, S. B.; Hop, C. E. C. A.; Wang, Z.; Strauss, J. R.; Cameron, P. M.; Nichols, E. A.; O'keefe, S. J.; O'neill, E. A.; Schmatz, D. M.; Schwartz, C. D.; Thompson, C. M.; Zaller, D. M.; Doherty, J. B. Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP Kinase. Bioorg. Med. Chem. Lett. 2003, 13, 277.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 277
-
-
Stelmach, J.E.1
Liu, L.2
Patel, S.B.3
Pivnichny, J.V.4
Scapin, G.5
Singh, S.B.6
Hop, C.E.C.A.7
Wang, Z.8
Strauss, J.R.9
Cameron, P.M.10
Nichols, E.A.11
O'keefe, S.J.12
O'Neill, E.A.13
Schmatz, D.M.14
Schwartz, C.D.15
Thompson, C.M.16
Zaller, D.M.17
Doherty, J.B.18
-
25
-
-
0037330941
-
P38 inhibitors: Piperidine and 4-aminopiperidine substituted naphthyridinones, quinolinones and dihydroquinazolinones
-
Hunt, J. A.; Kallashi, F.; Ruzek, R. D.; Sinclair, P. J.; Ita, I.; McCormick, S. X.; Pivnichny, J. V.; Hop, C. E. C. A.; Kumar, S.; Wang, Z.; O'Keefe, S. J.; O'Neill, E. A.; Porter, G.; Thompson, J. E.; Woods, A.; Zaller, D. M.; Doherty, J. B. P38 inhibitors: piperidine and 4-aminopiperidine substituted naphthyridinones, quinolinones and dihydroquinazolinones. Bioorg. Med. Chem. Lett. 2003, 13, 467.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 467
-
-
Hunt, J.A.1
Kallashi, F.2
Ruzek, R.D.3
Sinclair, P.J.4
Ita, I.5
McCormick, S.X.6
Pivnichny, J.V.7
Hop, C.E.C.A.8
Kumar, S.9
Wang, Z.10
O'Keefe, S.J.11
O'Neill, E.A.12
Porter, G.13
Thompson, J.E.14
Woods, A.15
Zaller, D.M.16
Doherty, J.B.17
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