College of Pharmacy, CHA University, Gyeonggi-do 11160, Republic of Korea.
College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
J Med Chem. 2020 Apr 23;63(8):3908-3914. doi: 10.1021/acs.jmedchem.9b01765. Epub 2020 Apr 1.
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 not only exhibited promising and potency but also exerted selective inhibition of H460 and A549 cells and AIMP2-DX2 rather than WI-26 cells and AIMP2. Aminophenylpyrimidine offers possible therapeutic potential in the treatment of lung cancer.
氨酰-tRNA 合成酶相互作用多功能蛋白 (AIMPs) 最近被认为是几种癌症的新的治疗靶点。在本出版物中，我们报告了新型 2-氨基苯基嘧啶作为新的 AIMP2-DX2 抑制剂的开发。特别是，氨基苯基嘧啶不仅表现出有希望的 和 效力，而且对 H460 和 A549 细胞以及 AIMP2-DX2 具有选择性抑制作用，而对 WI-26 细胞和 AIMP2 没有抑制作用。氨基苯基嘧啶在治疗肺癌方面可能具有潜在的治疗价值。
