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Steroidal nitrone inhibitors of 5α-reductase

✍ Scribed by Andrea J Robinson; Indawati DeLucca; Spencer Drummond; George A Boswell

Publisher
Elsevier Science
Year
2003
Tongue
French
Weight
106 KB
Volume
44
Category
Article
ISSN
0040-4039

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✦ Synopsis

This paper describes the rational design and synthesis of novel inhibitors of human steroid 5a-reductase. Steroidal nitrones were synthesised via an eight-step sequence from epiandrosterone and were tested for activity against type I and II 5a-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.

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