Structure-activity relationship studies and biological characterization of human NAD⁺-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors

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• 作者：Damien Y. Duveau ; Adam Yasgar ; Yuhong Wang ; Xin Hu ; Jennifer Kouznetsova ; Kyle R. Brimacombe ; Ajit Jadhav ; Anton Simeonov ; Craig J. Thomas ; David J. Maloney
• 关键词：HPGD ; 15-PGDH ; Prostaglandin ; PGE2 ; Inhibitor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 January, 2014
• 年：2014
• 卷：24
• 期：2
• 页码：630-635
• 全文大小：2177 K

文摘

The structure-activity relationship (SAR) study of two chemotypes identified as inhibitors of the human NAD⁺-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD, 15-PGDH) was conducted. Top compounds from both series displayed potent inhibition (IC₅₀ <50 nM), demonstrate excellent selectivity towards HPGD and potently induce PGE₂ production in A549 lung cancer and LNCaP prostate cancer cells.