| 词条 | Cytestrol acetate |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = (1S,10S,11S,14R,15S,17R)-17-(Acetyloxy)-5[bis(2-chloroethyl)carbamoyl]oxy14-ethynyl-15-methyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-2,4,6-trien-14-yl acetate | image = Cytestrol acetate.svg | width = 250px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = | CAS_supplemental = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID = 58838619 | UNII = | KEGG = | ChEBI = | ChEMBL = | synonyms = 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) | C=29 | H=35 | Cl=2 | N=1 | O=6 | SMILES = [H][C@@]12CC[C@@](OC(C)=O)(C#C)[C@@]1(C)C[C@@H](OC(C)=O)[C@]1([H])C3=CC=C(OC(=O)N(CCCl)CCCl)C=C3CC[C@@]21[H] | StdInChI_Ref = | StdInChI = 1S/C29H35Cl2NO6/c1-5-29(38-19(3)34)11-10-24-23-8-6-20-16-21(37-27(35)32(14-12-30)15-13-31)7-9-22(20)26(23)25(36-18(2)33)17-28(24,29)4/h1,7,9,16,23-26H,6,8,10-15,17H2,2-4H3/t23-,24-,25+,26+,28-,29-/m0/s1 | StdInChIKey_Ref = | StdInChIKey = RRJRVDYYFLBGSE-UPRLNUCLSA-N }}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
References1. ^1 2 3 {{cite journal|last1=Oborotov|first1=A. V.|last2=Smirnova|first2=Z. S.|last3=Osetrova|first3=I. P.|last4=Polozkova|first4=A. P.|last5=Rzheznikov|first5=V. M.|title=Antitumor activity of various medicinal forms of the new estrogenocytostatic drug cytestrol acetate|journal=Pharmaceutical Chemistry Journal|volume=33|issue=10|year=1999|pages=526–527|issn=0091-150X|doi=10.1007/BF02508372}} {{Estrogen receptor modulators}}{{Steroid-stub}}{{Antineoplastic-drug-stub}}2. ^1 2 3 {{cite journal | vauthors = Smirnova ZS, Rzheznikov VM, Tolkachev VN, Borisova LM, Kiseleva MP, Semeĭkin AV, Fedotcheva TA, Shirokikh KE, Banin VV, Shimanovskiĭ NL | title = [Antitumor and antiproliferative action of the steroidal cytostatic antiestrogen cytestrol acetate on hormone-dependent tumor models] | language = Russian | journal = Eksp Klin Farmakol | volume = 77 | issue = 10 | pages = 31–5 | year = 2014 | pmid = 25518525 | doi = | url = }} 3. ^1 2 3 Smirnova Z. S, (2003). [Experimental Study of Hormonocytostatics for Treatment of Breast Cancer.] Российский биотерапевтический журнал, 2(2). 4. ^1 2 Смирнова, З. С., Ржезников, В. М., Толкачев, В. Н., Борисова, Л. М., Киселева, М. П., Семейкин, А. В., ... & Шимановский, Н. Л. (2014). Противоопухолевое и антипролиферативное действие стероидного антиэстрогена цитэстрола ацетата на моделях гормонозависимых опухолей. Экспериментальная и клиническая фармакология, 77(10), 31-35. 10 : Acetate esters|Antiestrogens|Antineoplastic drugs|Carbamates|Hormonal antineoplastic drugs|Nitrogen mustards|Organochlorides|Prodrugs|Russian drugs|Chloroethyl compounds |
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