Norendoxifen
Norendoxifen, also known as N,N-didesmethyl-4-hydroxytamoxifen, 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]
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Other names | N,N-Didesmethyl-4-hydroxytamoxifen |
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Formula | C24H25NO2 |
Molar mass | 359.469 gยทmolโ1 |
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See also
- Afimoxifene (4-hydroxytamoxifen)
- Endoxifen (N-desmethyl-4-hydroxytamoxifen)
References
- Lu, Wenjie Jessie; Xu, Cong; Pei, Zifan; Mayhoub, Abdelrahman S.; Cushman, Mark; Flockhart, David A. (2012). "The tamoxifen metabolite norendoxifen is a potent and selective inhibitor of aromatase (CYP19) and a potential lead compound for novel therapeutic agents". Breast Cancer Res. Treat. 133 (1): 99โ109. doi:10.1007/s10549-011-1699-4. PMID 21814747.
- Lv, Wei; Liu, Jinzhong; Skaar, Todd C.; Flockhart, David A.; Cushman, Mark (2015). "Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities". J. Med. Chem. 58 (6): 2623โ48. doi:10.1021/jm501218e. PMC 4687028. PMID 25751283.
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