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

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 (K_i=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.