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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:24

Article

Duveau, Damien Y.¹  Yasgar, Adam¹  Wang, Yuhong¹  Hu, Xin¹  Kouznetsova, Jennifer¹  Brimacombe, Kyle R.¹  Jadhav, Ajit¹  Simeonov, Anton¹  Thomas, Craig J.¹  Maloney, David J.¹ 

[1] NIH, Natl Ctr Adv Translat Sci, Rockville, MD 20850 USA

关键词: HPGD;    15-PGDH;    Prostaglandin;    PGE(2);    Inhibitor;   

DOI  :  10.1016/j.bmcl.2013.11.081

来源: Elsevier

【 摘 要 】

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 PGE(2) production in A549 lung cancer and LNCaP prostate cancer cells. Published by Elsevier Ltd.

【 授权许可】

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