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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Chemical and physical data | |
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
- ^ Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 898–. ISBN 978-1-4757-2085-3.
- ^ a b Asai M, Takeuchi H, Okada H (January 1978). "In vivo interaction between steroidal alkylating agents and oestrogen receptors in rabbit uteri". Acta Endocrinologica. 87 (1): 173–180. doi:10.1530/acta.0.0870173. PMID 579532.
- ^ Leclercq G, Devleeschouwer N, Heuson JC (July 1983). James VH, Pasqualini JR (eds.). "Guide-lines in the design of new antiestrogens and cytotoxic-linked estrogens for the treatment of breast cancer". Journal of Steroid Biochemistry. 19 (1A). Elsevier Science: 75–85. doi:10.1016/S0022-4731(83)80009-0. ISBN 978-1-4831-9067-9. PMID 6887875.
- ^ Scullin P, O'Sullivan JM, Parker CC (5 September 2007). "Strategies for the Implementation of Chemotherapy". In Ablin RJ, Mason MD (eds.). Metastasis of Prostate Cancer. Springer Science & Business Media. pp. 311–. ISBN 978-1-4020-5847-9.
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- Estradiol (as a hormone)
- Estradiol (as a medication)
- Pharmacodynamics of estradiol
- Pharmacokinetics of estradiol
- Estrogen (as a hormone)
- Estrogen (as a medication)
- Menopausal hormone therapy
- Feminizing hormone therapy
- Estradiol-containing birth control pill
- Combined injectable birth control
- High-dose estrogen
- Hydroxylation of estradiol
- Estradiol acetate
- Estradiol acetylsalicylate
- Estradiol anthranilate
- Estradiol benzoate butyrate
- Estradiol benzoate cyclooctenyl ether
- Estradiol benzoate
- Estradiol butyrylacetate
- Estradiol cyclooctyl acetate
- Estradiol cypionate
- Estradiol decanoate
- Estradiol diacetate
- Estradiol dibutyrate
- Estradiol dienantate
- Estradiol dipropionate
- Estradiol distearate
- Estradiol disulfate
- Estradiol diundecylate
- Estradiol diundecylenate
- Estradiol enantate
- Estradiol furoate
- Estradiol glucuronide
- Estradiol hemisuccinate
- Estradiol hexahydrobenzoate
- Estradiol monopropionate
- Estradiol mustard
- Estradiol palmitate
- Estradiol phenylpropionate
- Estradiol phosphate
- Estradiol pivalate
- Estradiol propoxyphenylpropionate
- Estradiol salicylate
- Estradiol stearate
- Estradiol sulfamate
- Estradiol sulfate
- Estradiol undecylate
- Estradiol undecylenate
- Estradiol valerate
- Estramustine phosphate (estradiol normustine phosphate)
- Estrogen ester
- Polyestradiol phosphate
- Estrone
- Estriol
- Estetrol
- Ethinylestradiol
- Conjugated estrogens
- Esterified estrogens
- Estrone sulfate
- Estropipate (piperazine estrone sulfate)
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