Discovery of a novel hybrid from finasteride and epristeride as 5alpha-reductase inhibitor.

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Yao Z, Xu Y, Zhang M, Jiang S, Nicklaus MC, Liao C

Discovery of a novel hybrid from finasteride and epristeride as 5alpha-reductase inhibitor.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):475-8. doi: 10.1016/j.bmcl.2010.10.112. Epub 2010 Oct 28.

PubMed ID

21094046 [ View in PubMed

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Abstract

Finasteride and epristeride both inhibit 5alpha-reductase with high potency via competitive and non-competitive mechanism, respectively. A new hybrid of finasteride and epristeride was designed as a new 5alpha-reductase inhibitor based on combination principles in medicinal chemistry. Human 5beta-reductase was chosen as a plausible surrogate of 5alpha-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 5alpha-reductase inhibitor in low IC(50) ranges.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Finasteride	3-oxo-5-alpha-steroid 4-dehydrogenase 2	IC 50 (nM)	35	N/A	N/A	Details