Discovery of 2-((3-cyanopyridin-2-yl)thio)acetamides as human lactate dehydrogenase A inhibitors to reduce the growth of MG-63 osteosarcoma cells: Virtual screening and biological validation. Issue 16 (15th August 2016)

• Record Type: Journal Article
• Authors: Cui, Wei; Lv, Wei; Qu, Ying; Ma, Rui; Wang, Yi-Wei; Xu, Yong-Jun; Wu, Di; Chen, Xuanhuang
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 16(2016)
• Page Start: 3984
• Page End: 3987
• Publication Date: 2016-08-15
• Subjects: Lactate dehydrogenase A -- Virtual screening -- Apoptosis -- Cytotoxic assay; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.06.083
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Lactate dehydrogenase A (LDHA) has emerged as an attractive target in the oncology field. In this paper, we present the identification of 2-((3-cyanopyridin-2-yl)thio)acetamide-containing compounds as LDHA inhibitors. The in vitro enzymatic assay suggested that inhibitor9 had good inhibitory potency against LDHA with IC50 value as 1.24 μM. Cytotoxicity assay showed that inhibitor9 strongly inhibited the proliferation of cancer cell MG-63 (EC50 = 0.98 μM). These findings indicated that inhibitor9 could be employed as a lead for developing more potent LDHA inhibitor with anti-proliferative potency.