| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10592920 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
Activators of the pyruvate kinase M2 (PKM2) are currently attracting significant interest as potential anticancer therapies. They may achieve a novel antiproliferation response in cancer cells through modulation of the classic 'Warburg effect' characteristic of aberrant metabolism. In this Letter, we describe the optimization of a weakly active screening hit to a structurally novel series of small molecule 3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as potent PKM2 activators.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yong Xu, Xiao-Hui Liu, Michael Saunders, Scott Pearce, Jason M. Foulks, K. Mark Parnell, Adrianne Clifford, Rebecca N. Nix, Jeremy Bullough, Thomas F. Hendrickson, Kevin Wright, Michael V. McCullar, Steven B. Kanner, Koc-Kan Ho,