Design, synthesis, and structure activity relationship (SAR) studies of novel imidazo[1,2-a] pyridine derivatives as Nek2 inhibitors

Haili Wang, Yunzhong Chen, Xiaofan Gu, Jianbei Xi, Ziwei Ren, Shuting Wang, Yanhong Duan, Hongyu Li, Tong Zhu, Yijie Du, Xiongwen Zhang, Mingliang Ma

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

Never in mitosis (NIMA) related kinase 2 (Nek2) is involved in multiple cellular processes such as cell cycle checkpoint regulation, cell division, DNA damage response and cell apoptosis. Nek2 has been reported to be overexpressed in various tumors and correlated with poor prognosis. Herein, a series of imidazo[1,2-a] pyridines Nek2 inhibitors were designed, synthesized, and their biological activities were investigated. Besides, structure activity relationship analysis of these compounds were performed in the MGC-803 cell. The screening results are promising, and compound 28e shows good proliferation inhibitory activity with an IC50 of 38 nM. The results would be helpful to design and develop more effective Nek2 inhibitors for the treatment of gastric cancer.

Original languageEnglish (US)
Article number115775
JournalBioorganic and Medicinal Chemistry
Volume28
Issue number23
DOIs
StatePublished - Dec 1 2020
Externally publishedYes

Keywords

  • Antitumor activities
  • Gastric cancer
  • Imidazo[1,2-a]pyridine
  • Nek2

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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