Recently I am researching about BIOLOGICAL EVALUATION; MOLECULAR DOCKING; 20S PROTEASOME; DESIGN; DERIVATIVES; IDENTIFICATION; DEGRADATION; GENERATION; APOPTOSIS; MYELOMA, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC); Key Project of Zhejiang Provincial Natural Science Foundation of China; Science and Technology Commission of Shanghai MunicipalityScience & Technology Commission of Shanghai Municipality (STCSM); Strategic Priority Research Program of the Chinese Academy of SciencesChinese Academy of Sciences; National Major Scientific and Technological Special Project for Significant New Drugs Development. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Dong, XW; Zhang, JK; Xu, L; Che, JX; Cheng, G; Hu, XB; Sheng, L; Gao, AH; Li, J; Liu, T; Hu, YZ; Zhou, YB. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid. Category: Pyrazines
The potential of specific proteasome inhibitors to act as anti-cancer agents has attracted intensive investigations. The proteasome can be covalently inhibited by epoxyketone derivatives via a two-step reaction. Several computational approaches have been developed to mimic the covalent binding event. Compound 1 composed of a six-membered heterocyclic ring was designed by using covalent docking. With a possible different binding mode from the clinical compound Carfilzomib, it occupied the 55 pocket of 20S proteasome and showed favorable inhibitory activity. Subsequently optimization and evaluation were taken place. Among these compounds, 11h demonstrated extraordinary in vitro inhibitory activity and selectivity, and good in vivo proteasome inhibitory activity, a favorable pharmacokinetic profile and xenograft tumor inhibition. The possible binding pattern of compound 11h against proteasome was further fully explored via calculations, providing a theoretical basis for finding potent proteasome inhibitors. (C) 2018 Elsevier Masson SAS. All rights reserved.
Category: Pyrazines. Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.
Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem