Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds

被引：23

作者：

Dhar, T. G. Murali ^{[1
]}

Wrobleski, Stephen T. ^{[1
]}

Lin, Shuqun ^{[1
]}

Furch, Joseph A. ^{[1
]}

Nirschl, David S. ^{[1
]}

Fan, Yi ^{[1
]}

Todderud, Gordon ^{[1
]}

Pitt, Sidney ^{[1
]}

Doweyko, Arthur M. ^{[1
]}

Sack, John S. ^{[1
]}

Mathur, Arvind ^{[1
]}

McKinnon, Murray ^{[1
]}

Barrish, Joel C. ^{[1
]}

Dodd, John H. ^{[1
]}

Schieven, Gary L. ^{[1
]}

Leftheris, Katerina ^{[1
]}

机构：

[1] Bristol Myers Squibb Pharmaceut Res Inst, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 18期

关键词：

p38; alpha; MAP kinase inhibitors; TNF alpha; X-ray co-crystallography;

D O I：

10.1016/j.bmcl.2007.07.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and structure-activity relationships (SAR) of p38 alpha MAP kinase inhibitors based on heterobicyclic scaffolds are described. This effort led to the identification of compound (21) as a potent inhibitor of p38a MAP kinase with good cellular potency toward the inhibition of TNF-alpha production. X-ray co-crystallography of an oxalamide analog (24) bound to unphosphorylated p38 alpha is also disclosed. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：5019 / 5024

页数：6

共 50 条

[21] Synthesis and biological activity of quinolinone and dihydroquinolinone p38 MAP kinase inhibitors
Chen, Meng-Hsin
Fitzgerald, Patricia
Singh, Suresh B.
O'Neill, Edward A.
Schwartz, Cheryl D.
Thompson, Chris M.
O'Keefe, Stephen J.
Zaller, Dennis M.
Doherty, James B.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (06) : 2222 - 2226
[22] Design and synthesis of 4-azaindoles as inhibitors of p38 MAP kinase
Trejo, A
Arzeno, H
Browner, M
Chanda, S
Cheng, S
Comer, DD
Dalrymple, SA
Dunten, P
Lafargue, J
Lovejoy, B
Freire-Moar, J
Lim, J
Mcintosh, J
Miller, J
Papp, E
Reuter, D
Roberts, R
Sanpablo, F
Saunders, J
Song, K
Villasenor, A
Warren, SD
Welch, M
Weller, P
Whiteley, PE
Zeng, L
Goldstein, DM
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2003, 46 (22) : 4702 - 4713
[23] Identification of p38α MAP kinase inhibitors by pharmacophore based virtual screening
Gangwal, Rahul P.
Das, Nihar R.
Thanki, Kaushik
Damre, Mangesh V.
Dhoke, Gaurao V.
Sharma, Shyam S.
Jain, Sanyog
Sangamwar, Abhay T.
[J]. JOURNAL OF MOLECULAR GRAPHICS & MODELLING, 2014, 49 : 18 - 24
[24] Design, synthesis and SAR of bipyridine derivatives as potent and selective p38 kinase inhibitors
Tadesse, S
Hong, FT
Tamayo, N
Liao, L
Powers, D
Yudor, YY
Yu, V
Wong, M
Henkle, B
Middleton, S
Syed, R
Harvey, T
Hungate, R
Dominguez, C
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 230 : U2724 - U2724
[25] Synthesis and SAR of thienyl, furyl, and pyrrolyl urea p38 kinase inhibitors.
Scott, WJ
Redman, AM
Bhargava, A
Bombara, M
Caringal, Y
Dally, R
Dumas, J
Gunn, D
Housley, TJ
Kingery-Wood, J
Johnson, JS
Lee, W
Osterhout, M
Paulson, H
Popp, M
Ranges, GE
Renick, J
Schoenleber, R
Shrinkhande, A
Smith, RA
Swartz, S
Wild, H
Wilhelm, SM
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 222 : U684 - U684
[26] P38 α map kinase inhibitors:: From discovery to the clinic
Dugar, S
Mavunkel, B
Chakravarty, S
Perumattam, J
Luedtke, G
Lu, Q
Chen, Z
Xu, YJ
Protter, A
Schreiner, G
Almirez, R
Scott, B
Laney, M
Henson, M
Lewicki, J
Moore, A
Lee, S
Brahn, E
Liu, D
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 229 : U162 - U162
[27] p38 MAP kinase inhibitors: Progress, pitfalls and possibilities
Adams, JL
Gallagher, TF
Boehm, JC
Kassis, S
Gorycki, PD
Gum, RJ
Webb, EF
Sorenson, ME
Smietana, JM
Garigipati, RS
Hall, RF
Ayrton, A
Badger, A
Griswold, DE
Young, PR
Lee, JC
[J]. MEDICINAL CHEMISTRY INTO THE MILLENNIUM, 2001, (264): : 163 - 173
[28] New generation of p38 map kinase inhibitors.
Singh, S
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2003, 225 : U206 - U206
[29] p38 MAP Kinase Inhibitors as Anti inflammatory Agents
Amir, Mohammad
Somakala, K.
Ali, Sazid
[J]. MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2013, 13 (14) : 2082 - 2096
[30] Oxindolylidene derivatives as p38 MAP kinase inhibitors.
Cheng, S
Comer, DD
Freire-Moar, J
Goldstein, DM
Myers, PL
Saunders, J
Sjogren, EB
Teig, S
Warren, S
Whiteley, PE
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2000, 219 : U52 - U53

← 1 2 3 4 5 →