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Titolo:
Synthesis of (E)-4-[4,4-dimethyl-2,5-dioxo-3-{1 '-(125I)iodo-1 '-propen-3 '-yl}-1-imidazolidinyl]-2-trifluoromethylbenzonitrile: A potential radioligand for the androgen receptor
Autore:
Van Dort, ME; Hagen, CA;
Indirizzi:
Univ Michigan, Sch Med, Div Nucl Med, Dept Radiol, Ann Arbor, MI 48109 USAUniv Michigan Ann Arbor MI USA 48109 Dept Radiol, Ann Arbor, MI 48109 USA
Titolo Testata:
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
fascicolo: 1, volume: 44, anno: 2001,
pagine: 47 - 54
SICI:
0362-4803(200101)44:1<47:SO('''>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Keywords:
androgen receptor; iodine-125; iododestannylation; prostate cancer; RU 58841; single-photon emission computed tomography;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Physical, Chemical & Earth Sciences
Citazioni:
15
Recensione:
Indirizzi per estratti:
Indirizzo: Van Dort, ME Univ Michigan, Sch Med, Div Nucl Med, Dept Radiol, 3480 Kresge 3 Bldg, AnnArbor, MI 48109 USA Univ Michigan 3480 Kresge 3 Bldg Ann ArborMI USA 48109 9 USA
Citazione:
M.E. Van Dort e C.A. Hagen, "Synthesis of (E)-4-[4,4-dimethyl-2,5-dioxo-3-{1 '-(125I)iodo-1 '-propen-3 '-yl}-1-imidazolidinyl]-2-trifluoromethylbenzonitrile: A potential radioligand for the androgen receptor", J LABEL C R, 44(1), 2001, pp. 47-54

Abstract

The synthesis of a novel radioiodinated nonsteroidal androgen receptor ligand (E)-4-[4,4-dimethyl-2,5- -dioxo-3-{1'-(I-125)iodo-1'-propen-3'-yl}-1-imidazolidinyl]-2-trifluoromethylbenzonitrile ([I-125](1) under bar) is described. In vitro competitive binding studies demonstrated that (1) under bar bound to the rat androgen receptor with high affinity (Ki = 13 nM). No-carrier-added [1251](1) under bar was synthesized from the corresponding tri-n-butyltin precursor by an oxidative radioiododestannylation reaction with Na[I-125]iodide and 3% aqueous hydrogen peroxide as oxidant. Subsequent HPLC purification provided [I-125](1) under bar in 86-92% (average = 90%; n = 5)isolated radiochemical yields having >99% radiochemical and chemical purity and a specific activity range of 1574-1835 Ci/mmol (average = 1733 Ci/mmol; n = 3).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/02/20 alle ore 22:21:17