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Publication Detail

Title: N-Benzoyl anthranilic acid derivatives as selective inhibitors of aldo-keto reductase AKR1C3.

Authors: Sinreih, Maša; Sosič, Izidor; Beranič, Nataša; Turk, Samo; Adeniji, Adegoke O; Penning, Trevor M; Rižner, Tea Lanišnik; Gobec, Stanislav

Published In Bioorg Med Chem Lett, (2012 Sep 15)

Abstract: Human aldo-keto reductases AKR1C1-AKR1C3 are involved in the biosynthesis and inactivation of steroid hormones and prostaglandins and thus represent attractive targets for the development of new drugs. We synthesized a series of N-benzoyl anthranilic acid derivatives and tested their inhibitory activity on AKR1C enzymes. Our data show that these derivatives inhibit AKR1C1-AKR1C3 isoforms with low micromolar potency. In addition, five selective inhibitors of AKR1C3 were identified. The most promising inhibitors were compounds 10 and 13, with IC(50) values of 0.31 μM and 0.35 μM for AKR1C3, respectively.

PubMed ID: 22897946 Exiting the NIEHS site

MeSH Terms: 3-Hydroxysteroid Dehydrogenases/antagonists & inhibitors*; 3-Hydroxysteroid Dehydrogenases/metabolism; Aldo-Keto Reductase Family 1 Member C3; Dose-Response Relationship, Drug; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/chemistry; Enzyme Inhibitors/pharmacology*; Humans; Hydroxyprostaglandin Dehydrogenases/antagonists & inhibitors*; Hydroxyprostaglandin Dehydrogenases/metabolism; Models, Molecular; Molecular Structure; Stereoisomerism; Structure-Activity Relationship; ortho-Aminobenzoates/chemical synthesis; ortho-Aminobenzoates/chemistry; ortho-Aminobenzoates/pharmacology*

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