Author/Editor     Sinreih, Maša; Sosič, Izidor; Beranič, Nataša; Turk, Samo; Adeniji, Adegoke O; Penning, Trevor M; Lanišnik-Rižner, Tea; Gobec, Stanislav
Title     N-Benzoyl anthranilic acid derivatives as selective inhibitors of aldo/keto reductase AKR1C3
Type     članek
Source     Bioorg Med Chem Lett
Vol. and No.     Letnik 22, št. 18
Publication year     2012
Volume     str. 5948-51
Language     eng
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 IC50 values of 0.31 ?M and 0.35 ?M for AKR1C3, respectively.
Descriptors     ANTHRANILIC ACIDS
ALDEHYDE REDUCTASE
KETONE OXIDOREDUCTASES