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

…, Y Wang, X Hu, J Kouznetsova, KR Brimacombe…

Index: Duveau, Damien Y.; Yasgar, Adam; Wang, Yuhong; Hu, Xin; Kouznetsova, Jennifer; Brimacombe, Kyle R.; Jadhav, Ajit; Simeonov, Anton; Thomas, Craig J.; Maloney, David J. Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 2 p. 630 - 635

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Citation Number: 6

Abstract

Abstract 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 (IC 50< 50 nM), demonstrate excellent selectivity towards HPGD and potently induce PGE 2 production in A549 lung cancer and LNCaP prostate cancer cells.