Discovery of a novel hybrid from finasteride and epristeride as 5α-reductase inhibitor.
Bioorg Med Chem Lett
; 21(1): 475-8, 2011 Jan 01.
Article
in En
| MEDLINE
| ID: mdl-21094046
ABSTRACT
Finasteride and epristeride both inhibit 5α-reductase with high potency via competitive and non-competitive mechanism, respectively. A new hybrid of finasteride and epristeride was designed as a new 5α-reductase inhibitor based on combination principles in medicinal chemistry. Human 5ß-reductase was chosen as a plausible surrogate of 5α-reductase type II and the results indicate that although the hybrid compound possesses the main bulk of epristeride, its inhibitory mechanism is same as of finasteride. The hybrid turned out to be a potent 5α-reductase inhibitor in low IC(50) ranges.
Full text:
1
Database:
MEDLINE
Main subject:
3-Oxo-5-alpha-Steroid 4-Dehydrogenase
/
Finasteride
/
5-alpha Reductase Inhibitors
/
Androstadienes
Limits:
Humans
Language:
En
Year:
2011
Type:
Article