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Human lactate dehydrogenase A (LDHA) has been identified as a potential therapeutic target in the area of cancer metabolism. Herein, we report the discovery of novel LDHA inhibitors through docking-based virtual screening and biological assays. The primary enzymatic assay suggested that compound 11 targeted LDHA with an IC 50 value of 0.33 μM. The in vitro cytotoxic assay demonstrated that compound 11 reduced the growth of MG-63 cancer cells with an EC 50 value of 3.35 μM. Finally, we found that compound 11 induced the apoptosis of MG-63 cancer cells in a dose dependent manner, upregulated the oxygen consumption rate (OCR), and decreased the lactate formation and extracellular acidification rate (ECAR) in MG-63 cancer cells. Collectively, our data suggested that compound 11 could be a promising lead for the development of potent LDHA inhibitors.

Discovery of human lactate dehydrogenase A (LDHA) inhibitors as anticancer agents to inhibit the proliferation of MG-63 osteosarcoma cells