2-Aminophenylpyrimidines as Novel Inhibitors of Aminoacyl-tRNA Synthetase Interacting Multifunctional Protein 2 (AIMP2)-DX2 for Lung Cancer Treatment

  • J Med Chem. 2020 Apr 23;63(8):3908-3914. doi: 10.1021/acs.jmedchem.9b01765.
Seungbeom Lee  1  2 ,  Dae Gyu Kim  3 ,  Kyeojin Kim  2 ,  Taewoo Kim  1  2 ,  Semi Lim  3 ,  Hyejin Kong  1 ,  Sunghoon Kim  3  2 ,  Young-Ger Suh  1  2
Affiliations
  • 1. College of Pharmacy, CHA University, Gyeonggi-do 11160, Republic of Korea.
  • 2. College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
  • 3. Medicinal Bioconvergence Research Center, College of Pharmacy, Seoul National University, Seoul 08826, Korea.
PMID: 32208684 DOI: 10.1021/acs.jmedchem.9b01765
Abstract

Aminoacyl-tRNA Synthetase interacting multifunctional proteins (AIMPs) have recently been considered novel therapeutic targets in several cancers. In this publication we report the development of novel 2-aminophenylpyrimidines as new AIMP2-DX2 inhibitors. In particular, aminophenylpyrimidine 3 not only exhibited promising in vitro and in vivo potency but also exerted selective inhibition of H460 and A549 cells and AIMP2-DX2 rather than WI-26 cells and AIMP2. Aminophenylpyrimidine 3 offers possible therapeutic potential in the treatment of lung Cancer.