Design, synthesis and biological evaluation of novel aminopyrazole- and 7-azaindole-based Nek1 inhibitors and their effects on zebrafish kidney development

Bioorganic & Medicinal Chemistry Letters
2021.0

Abstract

NIMA-related protein kinase Nek1 is crucially involved in cell cycle regulation, DNA repair and microtubule regulation and dysfunctions of Nek1 play key roles in amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD) and several types of radiotherapy resistant cancer. Targeting of Nek1 could reveal a new class of radiosensitizing substances and provide useful tools to better understand the aforementioned diseases. In this report we explore substituted aminopyrazoles and 7-azaindoles as potent inhibitors for the Nek1 kinase domain and examine their effect on kidney organogenesis in Danio rerio.

Knowledge Graph

Similar Paper

Design, synthesis and biological evaluation of novel aminopyrazole- and 7-azaindole-based Nek1 inhibitors and their effects on zebrafish kidney development
Bioorganic & Medicinal Chemistry Letters 2021.0
Irreversible Nek2 Kinase Inhibitors with Cellular Activity
Journal of Medicinal Chemistry 2011.0
N -(1 H -Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1δ/ε inhibitors: Synthesis, biological evaluation and molecular modeling studies
Bioorganic & Medicinal Chemistry Letters 2017.0
Necrostatins regulate apoptosis, necroptosis, and inflammation in cisplatin-induced nephrotoxicity in LLC-PK1 cells
Bioorganic & Medicinal Chemistry Letters 2021.0
Synthesis and evaluation of novel 7-azaindazolyl-indolyl-maleimide derivatives as antitumor agents and protein kinase C inhibitors
Bioorganic & Medicinal Chemistry 2009.0
Discovery of Potent and Selective Inhibitors of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Protein Kinase as Potential Anticancer Agents
Journal of Medicinal Chemistry 2011.0
Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors
Journal of Medicinal Chemistry 2022.0
Synthesis and kinase inhibitory activity of novel substituted indigoids
Bioorganic & Medicinal Chemistry 2009.0
Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors
Bioorganic & Medicinal Chemistry Letters 2003.0
Synthesis and Antiproliferative Activity of 7-Azaindirubin-3′-oxime, a 7-Aza Isostere of the Natural Indirubin Pharmacophore
Journal of Natural Products 2009.0