Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369732 | Bioorganic & Medicinal Chemistry Letters | 2016 | 4 Pages |
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 inhibitor 9 had good inhibitory potency against LDHA with IC50 value as 1.24 μM. Cytotoxicity assay showed that inhibitor 9 strongly inhibited the proliferation of cancer cell MG-63 (EC50 = 0.98 μM). These findings indicated that inhibitor 9 could be employed as a lead for developing more potent LDHA inhibitor with anti-proliferative potency.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Wei Cui, Wei Lv, Ying Qu, Rui Ma, Yi-Wei Wang, Yong-Jun Xu, Di Wu, Xuanhuang Chen,