144026-74-4Relevant articles and documents
Optimization of ether and aniline based inhibitors of lactate dehydrogenase
Christov, Plamen P.,Kim, Kwangho,Jana, Somnath,Romaine, Ian M.,Rai, Ganesha,Mott, Bryan T.,Allweil, Alexander A.,Lamers, Alexander,Brimacombe, Kyle R.,Urban, Daniel J.,Lee, Tobie D.,Hu, Xin,Lukacs, Christine M.,Davies, Douglas R.,Jadhav, Ajit,Hall, Matthew D.,Green, Neal,Moore, William J.,Stott, Gordon M.,Flint, Andrew J.,Maloney, David J.,Sulikowski, Gary A.,Waterson, Alex G.
, (2021/04/12)
Lactate dehydrogenase (LDH) is a critical enzyme in the glycolytic metabolism pathway that is used by many tumor cells. Inhibitors of LDH may be expected to inhibit the metabolic processes in cancer cells and thus selectively delay or inhibit growth in transformed versus normal cells. We have previously disclosed a pyrazole-based series of potent LDH inhibitors with long residence times on the enzyme. Here, we report the elaboration of a new subseries of LDH inhibitors based on those leads. These new compounds potently inhibit both LDHA and LDHB enzymes, and inhibit lactate production in cancer cell lines.
SMALL MOLECULE INHIBITORS OF LACTATE DEHYDROGENASE AND METHODS OF USE THEREOF
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, (2016/07/27)
Provided is a compound of formula (I)[Formula (I) should be inserted here], in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/ or lactate dehydrogenase B (LDHB) activity in a cell.