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

作者：Cui, Wei; Lv, Wei; Qu, Ying; Ma, Rui; Wang, Yi-Wei; Xu, Yong-Jun; Wu, Di; Chen, Xuanhuang^*

来源：Bioorganic & Medicinal Chemistry Letters, 2016, 26(16): 3984-3987.

DOI：10.1016/j.bmcl.2016.06.083

• Lactate dehydrogenase A
• Virtual screening
• Apoptosis
• Cytotoxic assay

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 mu M. Cytotoxicity assay showed that inhibitor 9 strongly inhibited the proliferation of cancer cell MG-63 (EC50 = 0.98 mu M). These findings indicated that inhibitor 9 could be employed as a lead for developing more potent LDHA inhibitor with anti-proliferative potency.

• 出版日期2016-8-15
• 单位哈尔滨医科大学; 莆田学院; 黑龙江省医院