Discovery of benzodioxane analogues as lead candidates of AIMP2-DX2 inhibitors

Bo Ra Lee, Dae Gyu Kim, Young Mi Kim, Sunghoon Kim, Inhee Choi

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)


Aminoacyl-tRNA synthetase (ARS) interacting multifunctional protein2 (AIMP2) plays a vital role in protein synthesis. However, a splicing variant in which the second of the four exons of AIMP2 is deleted, inhibits the tumor suppression activity of AIMP2. Herein, we describe our discovery of series of potent AIMP2-DX2 inhibitors that are targeting lung cancer. Optimization of series using ligand-based drug design strategy led to discovery of compound 35, a potent AIMP2-DX2 inhibitor that is the most efficacious in H460 and A549 cells. This benzodioxane series may represent good starting points for further lead optimization of the identification potential drug candidates for the AIMP2-DX2 targeted treatment of lung cancer.

Original languageEnglish
Article number128889
JournalBioorganic and Medicinal Chemistry Letters
Publication statusPublished - 2022 Oct 1

Bibliographical note

Funding Information:
This work was supported by the National Research foundation of Korea (NRF) grant funded by the Korea government (MSIT)(NRF-2017M3A9G6068257, 2021R1A3B1076605). In addition, this research was supported by the Yonsei University Research Fund of 2021-22-0293, 2021-22-0291 and 2021-22-0061.

Publisher Copyright:
© 2022 Elsevier Ltd

All Science Journal Classification (ASJC) codes

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


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