HPLC of Formula: C2H4N4. In 2020.0 EUR J MED CHEM published article about BIOLOGICAL EVALUATION; AUTOPHAGY; APOPTOSIS; ROS; DESIGN in [Wang, Shuai; Ma, Xu-Bin; Yuan, Xiao-Han; Yu, Bin; Xu, Yi-Chao; Liu, Hong-Min] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China; [Wang, Shuai; Ma, Xu-Bin; Yuan, Xiao-Han; Yu, Bin; Xu, Yi-Chao; Liu, Hong-Min] Zhengzhou Univ, Key Lab Adv Drug Preparat Technol, Mil Educ, Zhengzhou 450001, Peoples R China; [Wang, Shuai] Massachusetts Gen Hosp, Gordon Ctr Med Imaging, Boston, MA 02129 USA; [Wang, Shuai] Harvard Med Sch, Boston, MA 02129 USA in 2020.0, Cited 33.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.
Mitochondria are known as powerhouse of cells and play the role of a bridge in redox balance, cell apoptosis, and autophagy. ROS accumulation can cause mitochondria damage, while the injured mitochondria will further enhance ROS levels reciprocally. Herein, we synthesized a novel series of [1,2,4] triazolo[1,5-a]pyrimidine-based compounds 4a-4v and tested their anti-proliferation efficacy against gastric cancer cell line MGC-803. Among them, compounds 4o and 4p inhibited gastric cancer cells at micromolar level. Compound 4o caused G2/M arrest and induced mitochondria-dependent apoptosis in MGC-803 and SGC-7901. However, inhibiting apoptosis pathway cannot prevent the inhibitory activity of compound 4o against gastric cancer cell. To our surprising, ROS level was increased by compound 4o and elevation of ROS could be rescued by NAC. In accordance with that, NAC absolutely prevented the anti-proliferation efficacy of compound 4o. We further found that autophagy inhibitor CQ rather than 3-MA partially reversed inhibitory activity of compound 4o in MGC-803 cells. Taken together, compound 4o exhibited its anti-proliferative activity via increasing ROS level and inducing autophagy, thus leading to apoptosis of gastric cancer cells. Therefore, compound 4o may support further development of lead compounds for gastric cancer therapy via mitochondria pathway. (C) 2020 Elsevier Masson SAS. All rights reserved.
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Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics