Synthesis and SAR of 2,4-diaminopyrimidines as potent c-jun N-terminal kinase inhibitors

被引：7

作者：

Song, Xinyi ^{[1
]}

He, Yuanjun ^{[1
]}

Koenig, Marcel ^{[1
]}

Shin, Youseung ^{[1
]}

Noel, Romain ^{[1
]}

Chen, Weimin ^{[1
]}

Ling, Yuan Yuan ^{[1
]}

Feurstein, Daniel ^{[1
]}

Lin, Li ^{[1
]}

Ruiz, Claudia H. ^{[1
]}

Cameron, Michael D. ^{[1
]}

Duckett, Derek R. ^{[1
]}

Kamenecka, Theodore M. ^{[1
]}

机构：

[1] Scripps Res Inst, Dept Mol Therapeut & Translat Res Inst, Jupiter, FL 33458 USA

来源：

MEDCHEMCOMM | 2012年 / 3卷 / 02期

关键词：

PROTEIN-KINASE; SIGNAL-TRANSDUCTION; ACTIVATION DOMAIN; PHOSPHORYLATION; STRESS; CARCINOMA; ATF-2; BINDS; JNK1;

D O I：

10.1039/c1md00219h

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The design and synthesis of a potent series of c-jun N-terminal kinase (JNK2) inhibitors is described. The development and optimization of the 2,4-diaminopyrimidines series was carried out from an earlier in-house kinase inhibitor program. Through the optimization of the scaffold 2, several cell potent compounds with good in vivo profiles were discovered.

引用

页码：238 / 243

页数：6

共 50 条

[21] c-Jun N-terminal kinase pathways in diabetes
Yang, Ruojing
Trevillyan, James M.
INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY, 2008, 40 (12): : 2702 - 2706
[22] c-Jun N-terminal kinase signaling in aging
Li, Yihao
You, Li
Nepovimova, Eugenie
Adam, Vojtech
Heger, Zbynek
Jomova, Klaudia
Valko, Marian
Wu, Qinghua
Kuca, Kamil
FRONTIERS IN AGING NEUROSCIENCE, 2024, 16
[23] Inhibitors of c-Jun N-Terminal Kinases: An Update
Koch, Pierre
Gehringer, Matthias
Laufer, Stefan A.
JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (01) : 72 - 95
[24] Signal transduction by the c-Jun N-terminal kinase
Davis, RJ
CELLULAR RESPONSES TO STRESS, 1999, (64): : 1 - 12
[25] Analysis of the interaction between c-Jun and c-Jun N-terminal kinase in vivo
May, GHW
Allen, KE
Clark, W
Funk, M
Gillespie, DAF
JOURNAL OF BIOLOGICAL CHEMISTRY, 1998, 273 (50) : 33429 - 33435
[26] Design, synthesis, and biological evaluation of bi-dentate c-Jun N-terminal kinase inhibitors
De, Surya K.
Stebbins, John L.
Chen, Vida
Purves, Angela
Megan, Riel-Mehan
Pellecchia, Maurizio
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2013, 245
[27] Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors
Jiang, Rong
Frackowiak, Bozena
Shin, Youseung
Song, Xinyi
Chen, Weimin
Lin, Li
Cameron, Michael D.
Duckett, Derek R.
Kamenecka, Theodore M.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (09) : 2683 - 2687
[28] C-Jun N-terminal kinase inhibitors: Structural insight into kinase-inhibitor complexes
Men Thi Hoai Duong
Lee, Joon-Hwa
Ahn, Hee-Chul
COMPUTATIONAL AND STRUCTURAL BIOTECHNOLOGY JOURNAL, 2020, 18 : 1440 - 1457
[29] Inhibition of c-Jun N-terminal kinase 1, but not c-Jun N-terminal kinase 2, suppresses apoptosis induced by ischemia/reoxygenation in rat cardiac myocytes
Hreniuk, D
Garay, M
Gaarde, W
Monia, BP
Mckay, RA
Cioffi, CL
MOLECULAR PHARMACOLOGY, 2001, 59 (04) : 867 - 874
[30] C-Jun N-Terminal Kinase 2 (JNK2) In Sepsis
Sala, M.
Gu, L.
Walter, J. M.
Chen, C.
Do-Umehara, H.
Zhang, Q.
Reyfman, P. A.
Anekalla, K.
Budinger, G. S.
Misharin, A. V.
Wunderink, R. G.
Liu, J.
AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE, 2017, 195

← 1 2 3 4 5 →