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

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2-Aminophenylpyrimidines as Novel Inhibitors of Aminoacyl-tRNA Synthetase Interacting Multifunctional Protein 2 (AIMP2)-DX2 for Lung Cancer Treatment.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-04-01 , 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 _{2,

3} , Young-Ger Suh _{1,

2}

Affiliation

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.

中文翻译：

2-氨基苯基嘧啶类药物是与氨酰基-tRNA合成酶相互作用的多功能蛋白2（AIMP2）-DX2的新型抑制剂，可用于肺癌治疗。

最近，氨酰基-tRNA合成酶相互作用多功能蛋白（AIMP）被认为是几种癌症的新型治疗靶标。在该出版物中，我们报道了作为新型AIMP2-DX2抑制剂的新型2-氨基苯基嘧啶的开发。特别地，氨基苯基嘧啶3不仅表现出有希望的体外和体内效力，而且还选择性抑制H460和A549细胞和AIMP2-DX2而不是WI-26细胞和AIMP2。氨基苯基嘧啶3在肺癌的治疗中可能提供治疗潜力。

更新日期：2020-04-24

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