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

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.

SUBMITTER: Duveau DY 

PROVIDER: S-EPMC3970110 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature

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

Duveau Damien Y DY   Yasgar Adam A   Wang Yuhong Y   Hu Xin X   Kouznetsova Jennifer J   Brimacombe Kyle R KR   Jadhav Ajit A   Simeonov Anton A   Thomas Craig J CJ   Maloney David J DJ  

Bioorganic & medicinal chemistry letters 20131204 2

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. ...[more]

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