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

  1. Author:
    Yao, Z. Y.
    Xu, Y. J.
    Zhang, M. M.
    Jiang, S.
    Nicklaus, M. C.
    Liao, C. Z.

  2. Author Address

    [Nicklaus, Marc C.; Liao, Chenzhong] NCI, Biol Chem Lab, Ctr Canc Res, NIH,DHHS, Frederick, MD 21702 USA. [Yao, Zhiyi; Xu, Yingjun; Zhang, Minmin; Jiang, Sheng] Shanghai Inst Technol, Coll Chem & Environm Engn, Shanghai 210032, Peoples R China. [Liao, Chenzhong] Nankai Univ, Coll Pharm, Tianjin 300071, Peoples R China.;Liao, CZ, NCI, Biol Chem Lab, Ctr Canc Res, NIH,DHHS, Frederick, MD 21702 USA.;chenzhongliao@yahoo.com
    1. Year: 2011
    2. Date: Jan
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 21
    2. 1
    3. Pages: 475-478
  4. Type of Article: Article
  5. ISSN: 0960-894X
  1. Abstract:

    Finasteride and epristeride both inhibit 5 alpha-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 5 beta-reductase was chosen as a plausible surrogate of 5 alpha-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 5 alpha-reductase inhibitor in low IC50 ranges. Published by Elsevier Ltd.

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External Sources

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  2. DOI: 10.1016/j.bmcl.2010.10.112
  3. View record in Web of Science®
  4. WOS: 000285544400098

Library Notes

  1. Fiscal Year: FY2010-2011
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