| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10592966 | Bioorganic & Medicinal Chemistry Letters | 2014 | 6 Pages |
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 (IC50 <50Â nM), demonstrate excellent selectivity towards HPGD and potently induce PGE2 production in A549 lung cancer and LNCaP prostate cancer cells.
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Authors
Damien Y. Duveau, Adam Yasgar, Yuhong Wang, Xin Hu, Jennifer Kouznetsova, Kyle R. Brimacombe, Ajit Jadhav, Anton Simeonov, Craig J. Thomas, David J. Maloney,