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

✍ Scribed by Zhiyi Yao; Yingjun Xu; Minmin Zhang; Sheng Jiang; Marc C. Nicklaus; Chenzhong Liao

Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
617 KB
Volume
21
Category
Article
ISSN
0960-894X

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✦ Synopsis

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

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