The development of a series of novel 4-substituted-2-aminopyrimidines as inhibitors of c-Jun N-terminal kinases is described. The synthesis, in vitro inhibitory values for JNK1, and the in vitro inhibitory value for a c-Jun cellular assay are discussed. Optimization of microsomal clearance led to the identification of 9c, whose kinase selectivity is reported.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2009.03.023 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Novel peptide inhibitor of matrix Metalloproteinases-1 from pufferfish skin collagen hydrolysates and its potential Photoprotective activity via the MAPK/AP-1 signaling pathway.
J Photochem Photobiol B
December 2024
Fisheries Research Institute of Fujian, National Research and Development Center for Marine Fish Processing, Key Laboratory of Cultivation and High-value Utilization of Marine Organisms in Fujian Province, Xiamen, China. Electronic address:
Takifugu bimaculatus, a pufferfish species farmed in Fujian Province, is known for its non-toxic flesh and collagen-rich skin. We identified a novel collagen-derived matrix metalloproteinase 1 (MMP-1) inhibitory peptide, from T. bimaculatus skin with potent anti-photoaging properties.
View Article and Find Full Text PDFThe JNK Signaling Pathway Regulates Seizures Through ENT1 in Pilocarpine-Induced Epilepsy Rat Model.
CNS Neurosci Ther
December 2024
The Collaborative Innovation Center of Tissue Damage Repair and Regeneration Medicine of Zunyi Medical University, Zunyi, Guizhou, China.
Objective: The study investigates whether the expression and function of ENT1 can be regulated by inhibiting the JNK signaling pathway, thereby altering the levels of extracellular adenosine and glutamate in neurons, and subsequently affecting the progression of epilepsy.
Methods: The adult male SD rats were randomly divided into four groups: EP + SP600125 group, EP + DMSO group, EP group, and normal control group. The expression levels of ENT1, p-JNK, and JNK in the hippocampus of rats from each experimental group were detected using Western blotting technology.
Caffeic Acid Phenethyl Ester Enhances Bone Repair-related Factors in MC3T3-E1 Cells.
Cell Biochem Biophys
December 2024
Department of Regenerative Dental Medicine, Tokushima University Graduate School of Biomedical Sciences, 3-18-15 Kuramoto-cho, Tokushima, 770-8504, Japan.
Apical periodontitis is an inflammatory disease caused by bacterial infection in the root canal that spreads to the apical periodontal tissues, resulting in bone resorption around the root apex as the disease progresses. Vascular endothelial growth factor (VEGF), a growth factor involved in angiogenesis, plays an important role in bone remodeling. We reported that caffeic acid phenethyl ester (CAPE), a bioactive substance of propolis, induces VEGF in odontoblast-like cells and dental pulp cells.
View Article and Find Full Text PDFPiperine induces cellular stresses, apoptosis, and cytotoxicity via JNK signaling and has concentration-dependently additive or synergistic effects with sorafenib in hepatocellular carcinoma: an in-vitro study.
Naunyn Schmiedebergs Arch Pharmacol
December 2024
Department of Medical Biochemistry, Trakya University School of Medicine, Edirne, 22030, Turkey.
We aimed to determine the effects of piperine on cell viability, cellular stresses, and apoptosis first, then the relationship of piperine's effects with the c-Jun N-terminal kinase (JNK) signaling pathway, and also the interaction of piperine with sorafenib in hepatocellular carcinoma. Hepatocellular carcinoma (HepG2 and Hep3B) and non-cancerous hepatocyte (AML12) cell lines were used. The cell viability was determined by using MTT assay.
View Article and Find Full Text PDF[Protective effect of Polygonati Rhizoma aqueous extract on gastric mucosal injury in mice induced by overtaking pungent substances and alcohol via TRAF1/ASK1/JNK pathway].
Zhongguo Zhong Yao Za Zhi
October 2024
School of Pharmaceutical Sciences, Zhejiang Chinese Medical University Hangzhou 310053, China.
This study aims to investigate the effect and potential mechanism of Polygonati Rhizoma aqueous extract in protecting mice from gastric mucosal injury(stomach Yin deficiency). ICR mice were administrated with the mixture of pungent substance extract and alcohol by gavage once a day for 6 weeks to establish the mouse model of gastric mucosal injury with gastric Yin deficiency. The modeled mice were randomized into three groups of model and Polygonati Rhizoma aqueous extract administrated at 0.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!