Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors

被引：23
作者：
Shin, Youseung
Chen, Weiming
Habel, Jeff
Duckett, Derek
Ling, Yuan Yuan
Koenig, Marcel
He, Yuanjun
Vojkovsky, Tomas
LoGrasso, Philip [1 ]
Kamenecka, Theodore M.
机构：
[1] Scripps Res Inst, Dept Mol Therapeut, Jupiter, FL 33458 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 12期
关键词：
JNK; Kinase; ACTIVATED PROTEIN-KINASES; SELECTIVE INHIBITORS; DESIGN; POTENT; INFLAMMATION; APOPTOSIS; ASTHMA;
D O I：
10.1016/j.bmcl.2009.03.086
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel series of c-jun N-terminal kinase (JNK) inhibitors were designed and developed from a high-throughput-screening hit. Through the optimization of the piperazine amide 1, several potent compounds were discovered. The X-ray crystal structure of 4g showed a unique binding mode different from other well known JNK3 inhibitors. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3344 / 3347
页数：4
相关论文
共 50 条
[21]   C-Jun N-terminal kinase (JNK) isoforms play differing roles in otitis media [J].
Yao, William ;
Frie, Meredith ;
Pan, Jeffrey ;
Pak, Kwang ;
Webster, Nicholas ;
Wasserman, Stephen I. ;
Ryan, Allen F. .
BMC IMMUNOLOGY, 2014, 15
[22]   C-Jun N-terminal kinase inhibitors: Structural insight into kinase-inhibitor complexes [J].
Men Thi Hoai Duong ;
Lee, Joon-Hwa ;
Ahn, Hee-Chul .
COMPUTATIONAL AND STRUCTURAL BIOTECHNOLOGY JOURNAL, 2020, 18 :1440-1457
[23]   C-Jun N-terminal kinase signalling pathway in response to cisplatin [J].
Yan, Dong ;
An, GuangYu ;
Kuo, Macus Tien .
JOURNAL OF CELLULAR AND MOLECULAR MEDICINE, 2016, 20 (11) :2013-2019
[24]   The Role of c-Jun N-Terminal Kinase (JNK) in Retinal Degeneration and Vision Loss [J].
Kim, Byung-Jin ;
Zack, Donald J. .
RETINAL DEGENERATIVE DISEASES: MECHANISMS AND EXPERIMENTAL THERAPY, 2018, 1074 :351-357
[25]   c-Jun N-Terminal Kinase is Upregulated in Patients With Hypospadias [J].
Li, Mingyong ;
Qiu, Lin ;
Lin, Tao ;
He, Dawei ;
Hua, Yi ;
Yuan, Xingang ;
Liu, Xing ;
Wei, Guanghui .
UROLOGY, 2013, 81 (01) :178-183
[26]   Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies [J].
Liu, Mei ;
Wang, Sanyi ;
Clampit, Jill E. ;
Gum, Rebecca J. ;
Haasch, Deanna L. ;
Rondinone, Cristina M. ;
Trevillyan, James M. ;
Abad-Zapatero, Cele ;
Fry, Elizabeth H. ;
Sham, Hing L. ;
Liu, Gang .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (03) :668-672
[27]   Discovery of 2-(5-nitrothiazol-2-ylthio) benzo[d] thiazoles as novel c-Jun N-terminal kinase inhibitors [J].
De, Surya K. ;
Chen, Li-Hsing ;
Stebbins, John L. ;
Machleidt, Thomas ;
Riel-Mehan, Megan ;
Dahl, Russell ;
Chen, Vida ;
Yuan, Hongbin ;
Barile, Elisa ;
Emdadi, Aras ;
Murphy, Ria ;
Pellecchia, Maurizio .
BIOORGANIC & MEDICINAL CHEMISTRY, 2009, 17 (07) :2712-2717
[28]   c-Jun N-terminal kinase pathways in diabetes [J].
Yang, Ruojing ;
Trevillyan, James M. .
INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY, 2008, 40 (12) :2702-2706
[29]   c-Jun N-terminal kinase signaling in aging [J].
Li, Yihao ;
You, Li ;
Nepovimova, Eugenie ;
Adam, Vojtech ;
Heger, Zbynek ;
Jomova, Klaudia ;
Valko, Marian ;
Wu, Qinghua ;
Kuca, Kamil .
FRONTIERS IN AGING NEUROSCIENCE, 2024, 16
[30]   c-Jun N-terminal kinase 2 suppresses pancreatic cancer growth and invasion and is opposed by c-Jun N-terminal kinase 1 [J].
Tian, Xiaodong ;
Traub, Benno ;
Shi, Jingwei ;
Huber, Nadine ;
Schreiner, Stefan ;
Chen, Guowei ;
Zhou, Shaoxia ;
Henne-Bruns, Doris ;
Knippschild, Uwe ;
Kornmann, Marko .
CANCER GENE THERAPY, 2022, 29 (01) :73-86
12345