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Design, synthesis and biological evaluation of novel aminopyrazole- and 7-azaindole-based Nek1 inhibitors and their effects on zebrafish kidney development.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Dec 01; Vol. 53, pp. 128418. Date of Electronic Publication: 2021 Oct 26. - Publication Year :
- 2021
-
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.<br /> (Copyright © 2021 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Dose-Response Relationship, Drug
Indoles chemical synthesis
Indoles chemistry
Kidney growth & development
Kidney metabolism
Molecular Structure
NIMA-Related Kinase 1 metabolism
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors chemistry
Pyrazoles chemical synthesis
Pyrazoles chemistry
Structure-Activity Relationship
Zebrafish
Drug Design
Indoles pharmacology
Kidney drug effects
NIMA-Related Kinase 1 antagonists & inhibitors
Protein Kinase Inhibitors pharmacology
Pyrazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 53
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 34715306
- Full Text :
- https://doi.org/10.1016/j.bmcl.2021.128418