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Anticancers, Hormonals & Metabolic Disease Therapy

Hormone Therapy/5-α-Reductase Inhibitors: Novel 5-α-Reductase Inhibitors which Do not Contain the 4-aza Group

Pages 605-607 | Published online: 02 Mar 2011
 

Summary

Novelty: Novel carboxyl and carboxyl ester substituted 7-keto and hydroxy analogues of synthetic steroidal compounds are claimed. These compounds are mammalian steroid 5-α-reductase inhibitors, and are useful in the preparation of medicaments for reducing prostate size.

Biology: In vitro human prostatic steroid 5-α-reductase inhibition data are presented for three selected compounds (Ki=4 to 45 nM).

Chemistry: These analogues are prepared in a three-step synthesis. 17β-(N,N-Diisopropylcarboxamido)-7β-hydroxy-androsta-3,5-diene-3-carboxylic acid is the most active compound of the three compounds which are specifically claimed.

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