Author/Authors :
Robinson، نويسنده , , Andrea J and DeLucca، نويسنده , , Indawati and Drummond، نويسنده , , Spencer and Boswell، نويسنده , , George A، نويسنده ,
Abstract :
This paper describes the rational design and synthesis of novel inhibitors of human steroid 5α-reductase. Steroidal nitrones were synthesised via an eight-step sequence from epiandrosterone and were tested for activity against type I and II 5α-reductase isozymes. Judicious placement of the nitrone into the steroid A-ring provided an effective and stable transition-state mimic of the postulated enolate intermediate involved in the conversion of testosterone into dihydrotestosterone.
