Chemistry:Norendoxifen
From HandWiki
Short description: Chemical compound
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| Other names | 4-Hydroxy-N,N-didesmethyltamoxifen |
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| Formula | C24H25NO2 |
| Molar mass | 359.469 g·mol−1 |
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Norendoxifen, also known as 4-hydroxy-N,N-didesmethyltamoxifen, is a nonsteroidal aromatase inhibitor (AI) of the triphenylethylene group that was never marketed.[1] It is an active metabolite of the selective estrogen receptor modulator (SERM) tamoxifen.[1] Unlike tamoxifen, norendoxifen is not a SERM, and instead has been found to act as a potent and selective competitive inhibitor of aromatase (Ki = 35 nM).[1] Drugs with dual SERM and AI activity, such as 4'-hydroxynorendoxifen, have been developed from norendoxifen, and may have therapeutic potential as antiestrogens in the treatment of estrogen receptor-positive breast cancer.[2]
See also
- Afimoxifene (4-hydroxytamoxifen)
- Endoxifen (4-hydroxy-N-desmethyltamoxifen)
References
- ↑ 1.0 1.1 1.2 "The tamoxifen metabolite norendoxifen is a potent and selective inhibitor of aromatase (CYP19) and a potential lead compound for novel therapeutic agents". Breast Cancer Research and Treatment 133 (1): 99–109. May 2012. doi:10.1007/s10549-011-1699-4. PMID 21814747.
- ↑ "Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities". Journal of Medicinal Chemistry 58 (6): 2623–48. March 2015. doi:10.1021/jm501218e. PMID 25751283.
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