2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
M. Walsh,K. Brimacombe,10 Authors,M. Boxer
2011 · DOI: 10.1016/j.bmcl.2011.08.114
Bioorganic & Medicinal Chemistry Letters · 66 Citations
TLDR
The third chemotype in a series of PKM2 activators based on the 2-oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamide scaffold is reported, and the synthesis, structure activity relationships, selectivity and notable physiochemical properties are described.