In 2017,Crowley, Vincent M.; Huard, Dustin J. E.; Lieberman, Raquel L.; Blagg, Brian S. J. published 《Second Generation Grp94-Selective Inhibitors Provide Opportunities for the Inhibition of Metastatic Cancer》.Chemistry – A European Journal published the findings.Synthetic Route of C6H4BrNO The information in the text is summarized as follows:
Glucose regulated protein 94 (Grp94) is the endoplasmic reticulum (ER) resident isoform of the 90-kDa heat shock protein (Hsp90) family and its inhibition represents a promising therapeutic target for the treatment of many diseases. Modification of the first generation cis-amide bioisostere imidazole to alter the angle between the resorcinol ring and the benzyl side chain via cis-amide replacements produced compounds with improved Grp94 affinity and selectivity. Structure-activity relationship studies led to the discovery of compound 30 (Me 3-chloro-2-(2-(4-fluorobenzyl)phenethyl)-4,6-dihydroxybenzoate), which exhibits 540 nM affinity and 73-fold selectivity towards Grp94. Grp94 is responsible for the maturation and trafficking of proteins associated with cell signaling and motility, including select integrins. The Grp94-selective inhibitor 30 was shown to exhibit potent anti-migratory effects against multiple aggressive and metastatic cancers.2-Bromonicotinaldehyde(cas: 128071-75-0Synthetic Route of C6H4BrNO) was used in this study.
2-Bromonicotinaldehyde(cas: 128071-75-0) belongs to pyridine. Pyridines form stable salts with strong acids. Pyridine itself is often used to neutralize acid formed in a reaction and as a basic solvent. Synthetic Route of C6H4BrNO