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

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

  • Bioorg Med Chem Lett. 2021 Dec 1;53:128418. doi: 10.1016/j.bmcl.2021.128418.
Johannes Pilakowski 1,  Georg Baumann 1,  Yung-Hsin Shih 1,  Tobias Meckel 2,  Boris Schmidt 3
Affiliations

Affiliations

  • 1 Clemens-Schöpf-Institute of Organic Chemistry and Biochemistry, Technische Universität Darmstadt, 64287 Darmstadt, Germany.
  • 2 Ernst-Berl-Institute, Group of Macromolecular Chemistry and Paper Chemistry, Technische Universität Darmstadt, 64287 Darmstadt, Germany.
  • 3 Clemens-Schöpf-Institute of Organic Chemistry and Biochemistry, Technische Universität Darmstadt, 64287 Darmstadt, Germany. Electronic address: schmidt_boris@mac.com.
PMID: 34715306 DOI: 10.1016/j.bmcl.2021.128418
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.

Keywords

7-Azaindole; Aminopyrazole; Nek1; Polycystic kidney disease; Zebrafish.

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