Patent Number: 9,649,305

Title: PFKFB3 inhibitor and methods of use as an anti-cancer therapeutic

Abstract: A novel compound, (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one- , is provided herein. (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) with surprisingly superior efficacy and pharmacodynamic properties in vitro and in vivo. Also provided are pharmaceutical compositions including the compound and methods of use of the compound in treating cancer and tumors in vivo, as well as inhibiting glycolytic flux and PFKFB3 enzymatic activity in cells. ##STR00001##

Inventors: Tapolsky; Gilles H. (Louisville, KY), Chand; Pooran (Birmingham, AL)

Assignee: Advanced Cancer Therapeutics, LLC

International Classification: A61K 31/00 (20060101); A61K 31/235 (20060101); C07C 311/13 (20060101); C07D 401/06 (20060101); A61K 31/4709 (20060101); A61K 45/06 (20060101)

Expiration Date: 2021-05-16 0:00:00