Chemistry:Estradiol mustard
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| Other names | NSC-112259; Estradiol 3,17β-bis(4-(bis(2-chloroethyl)amino)phenyl)acetate |
| Drug class | Chemotherapeutic agent; Estrogen; Estrogen ester |
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| Formula | C42H50Cl4N2O4 |
| Molar mass | 788.67 g·mol−1 |
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Estradiol mustard, also known as estradiol 3,17β-bis(4-(bis(2-chloroethyl)amino)phenyl)acetate, is a semisynthetic, steroidal estrogen and cytostatic antineoplastic agent and a phenylacetic acid nitrogen mustard-coupled estrogen ester that was never marketed.[1] It is selectively distributed into estrogen receptor (ER)-positive tissues such as ER-expressing tumors like those seen in breast and prostate cancers.[2] For this reason, estradiol mustard and other cytostatic-linked estrogens like estramustine phosphate have reduced toxicity relative to non-linked nitrogen mustard cytostatic antineoplastic agents.[2] However, they may stimulate breast tumor growth due to their inherent estrogenic activity and are said to be devoid of major therapeutic efficacy in breast cancer,[3] although estramustine phosphate has been approved for and is used (almost exclusively) in the treatment of prostate cancer.[4]
See also
References
- ↑ The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014. pp. 898–. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA898.
- ↑ 2.0 2.1 "In vivo interaction between steroidal alkylating agents and oestrogen receptors in rabbit uteri". Acta Endocrinologica 87 (1): 173–180. January 1978. doi:10.1530/acta.0.0870173. PMID 579532.
- ↑ "Guide-lines in the design of new antiestrogens and cytotoxic-linked estrogens for the treatment of breast cancer". Journal of Steroid Biochemistry (Elsevier Science) 19 (1A): 75–85. July 1983. doi:10.1016/S0022-4731(83)80009-0. ISBN 978-1-4831-9067-9. PMID 6887875. https://books.google.com/books?id=1VMJAwAAQBAJ&pg=PA75.
- ↑ "Strategies for the Implementation of Chemotherapy". Metastasis of Prostate Cancer. Springer Science & Business Media. 5 September 2007. pp. 311–. ISBN 978-1-4020-5847-9. https://books.google.com/books?id=AAo2qVvcVJcC&pg=PA311.
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