Jia, Cong-Cong;Chen, Wang;Feng, Zi-Li;Liu, Zhao-Peng published 《Recent developments of RET protein kinase inhibitors with diverse scaffolds as hinge binders》. The research results were published in《Future Medicinal Chemistry》 in 2021.COA of Formula: C6H4N2 The article conveys some information:
A review. RET is a proto-oncogene encoding a receptor tyrosine kinase. RET regulates key aspects of cellular proliferation, differentiation and survival. The activation of RET via gene fusions or point mutations is closely related to lung, thyroid and other cancers. This review summarizes the developments of a diversity of small mol. RET protein kinase inhibitors in the past 10 years. These RET inhibitors are classified according to their hinge binder chemotypes as: pyrimidines, including the pyrazolopyrimidines, pyrimidine oxazines, quinazolines, 4-aminopyrimidines and 4-aminopyridines; indolinones; 5-aminopyrazole-4-carboxamides; 3-trifluoromethylanilines; imidazopyridines, imidazopyridazines and pyrazopyridines; nicotinonitriles; pyridones and 1,2,4-triazoles. In each section, the biol. activities of the inhibitors, their structure-activity relationships and possible binding modes with the RET kinase are introduced. The experimental procedure involved many compounds, such as 3-Cyanopyridine (cas: 100-54-9) .
3-Cyanopyridine(cas: 100-54-9) has been shown to have a number of pharmacological effects: it inhibits the production of prostaglandin E2 and nitric oxide in congestive heart failure patients; it prevents the formation of diazonium salt from benzene and nitrogen dioxide; it inhibits the growth of tumor cell lines; and it protects mice from radiation injury by scavenging reactive oxygen species. COA of Formula: C6H4N2