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Bioorg Med Chem Lett. 2014 Jan 15;24(2):630-5. doi: 10.1016/j.bmcl.2013.11.081. Epub 2013 Dec 4.

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

Author information

1
National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, United States.
2
National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, United States. Electronic address: maloneyd@mail.nih.gov.

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 <50 nM), demonstrate excellent selectivity towards HPGD and potently induce PGE2 production in A549 lung cancer and LNCaP prostate cancer cells.

KEYWORDS:

15-PGDH; HPGD; Inhibitor; PGE(2); Prostaglandin

PMID:
24360556
PMCID:
PMC3970110
DOI:
10.1016/j.bmcl.2013.11.081
[Indexed for MEDLINE]
Free PMC Article

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