Chemistry:Cytestrol acetate
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| Other names | 11α-Hydroxyethinylestradiol 3-(bis(2-chloroethyl)carbamate) 11α,17β-diacetate; 17α-Ethynylestra-1,3,5(10)-triene-3,11α,17β-triol 11α,17β-diacetate 3-(bis(2-chloroethyl)carbamate) |
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| Chemical and physical data | |
| Formula | C29H35Cl2NO6 |
| Molar mass | 564.50 g·mol−1 |
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Cytestrol acetate is a steroidal antiestrogen and a cytostatic antineoplastic agent (i.e., chemotherapeutic) which was developed for the treatment of breast cancer but was never marketed.[1][2][3][4]
It is an 11α-hydroxylated derivative of ethinylestradiol in which a bis(2-chloroethyl)amine nitrogen mustard moiety has been attached as an ester at the C3 position and acetate esters have been attached at the C11α and C17β positions.[1][2][3][4] The mechanism of action of cytestrol acetate in breast cancer is two-fold: (1) acting as an antiestrogen similarly to fulvestrant or ICI-164384; and (2) having cytostatic actions via the carbamate–nitrogen mustard moiety analogously to estramustine phosphate.[1][2][3][4] The drug shows potent efficacy against breast cancer superior to that of tamoxifen in in vitro models.[1][2][3]
See also
- World War II
References
- ↑ 1.0 1.1 1.2 1.3 "Antitumor activity of various medicinal forms of the new estrogenocytostatic drug cytestrol acetate". Pharmaceutical Chemistry Journal 33 (10): 526–527. 1999. doi:10.1007/BF02508372. ISSN 0091-150X.
- ↑ 2.0 2.1 2.2 2.3 "[Antitumor and antiproliferative action of the steroidal cytostatic antiestrogen cytestrol acetate on hormone-dependent tumor models]" (in ru). Eksperimental'naia i Klinicheskaia Farmakologiia 77 (10): 31–35. 2014. PMID 25518525.
- ↑ 3.0 3.1 3.2 3.3 "[Experimental Study of Hormonocytostatics for Treatment of Breast Cancer.]" (in Russian). Российский биотерапевтический журнал 2 (2). 2003.
- ↑ 4.0 4.1 4.2 "Противоопухолевое и антипролиферативное действие стероидного антиэстрогена цитэстрола ацетата на моделях гормонозависимых опухолей." (in Russian). Экспериментальная и клиническая фармакология 77 (10): 31–35. November 2014.
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