An article Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators WOS:000573916100021 published article about CELL-DEATH; ENDOPLASMIC-RETICULUM; DUAL ROLES; APOPTOSIS; EXPRESSION; STRESS; UBIQUITINATION; METABOLISM; ACTIVATION; INDUCTION in [Li, Baicun; Yao, Jie; Guo, Kaiqiang; He, Fengming; Chen, Kun; Lin, Zongxin; Liu, Shunzhi; Huang, Jiangang; Wu, Qiaoqiong; Fang, Meijuan; Zeng, Jinzhang; Wu, Zhen] Xiamen Univ, Sch Pharmaceut Sci, Fujian Prov Key Lab Innovat Drug Target Res, Xiamen 361102, Peoples R China; [Li, Baicun; Yao, Jie; Guo, Kaiqiang; He, Fengming; Chen, Kun; Lin, Zongxin; Liu, Shunzhi; Huang, Jiangang; Wu, Qiaoqiong; Fang, Meijuan; Zeng, Jinzhang; Wu, Zhen] Xiamen Univ, Sch Pharmaceut Sci, State Key Lab Cellular Stress Biol, Xiamen 361102, Peoples R China; [Li, Baicun] Chinese Acad Med Sci, Inst Basic Med Sci, Dept Physiol, State Key Lab Med Mol Biol, Beijing 100005, Peoples R China; [Li, Baicun] Peking Union Med Coll, Sch Basic Med, Beijing 100005, Peoples R China in 2020.0, Cited 74.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Computed Properties of C6H5NO
Nur77 is a potential target for the treatment of cancer such as HCC. Herein, we detailed the discovery of a novel series of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as potential Nur77 modulators. The studies of antiproliferative activity and Nur77-binding affinity of target compounds resulted in the discovery of a lead candidate (10g), which was a good Nur77 binder (K-D = 3.58 +/- 0.16 mu M) with a broad-spectrum antiproliferative activity against all tested hepatoma cells (IC50 < 2.0 mu M) and was low toxic to normal LO2 cells. 10g could up-regulate Nur77 expression and mediate sub-cellular localization of Nur77 to induce apoptosis in hepatocellular carcinoma cell lines, which relied on 10g inducing Nur77-dependent autophagy and endoplasmic reticulum stress as the upstream of apoptosis. Moreover, the in vivo assays verified that 10g significantly inhibited xenograft tumor growth. These results indicate that 10g has the potential to be developed as a novel Nur77-targeting anti-hepatoma drug. (C) 2020 Elsevier Masson SAS. All rights reserved. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Li, BC; Yao, J; Guo, KQ; He, FM; Chen, K; Lin, ZX; Liu, SZ; Huang, JG; Wu, QQ; Fang, MJ; Zeng, JZ; Wu, Z or concate me.. Computed Properties of C6H5NO
Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem