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Titolo:
Synthesis and biological evaluation of two new radiolabelled estrogens: [I-125](E)-3-methoxy-17 alpha-iodovinylestra-1,3,5(10),6-tetraen-17 beta-ol and [I-125](Z)-3-methoxy-17 alpha-iodovinylestra-1,3,5(10),6-tetraen-17 beta-ol
Autore:
Silva, MCME; Patricio, L; Gano, L; Melo, MLSE; Inohae, E; Mataka, S; Thiemann, T;
Indirizzi:
Inst Tecnol & Nucl, P-2685 Sacavem, Portugal Inst Tecnol & Nucl Sacavem Portugal P-2685 ucl, P-2685 Sacavem, Portugal Univ Coimbra, Ctr Estudos Farmaceut, Fac Farm, P-3000 Coimbra, Portugal Univ Coimbra Coimbra Portugal P-3000 Fac Farm, P-3000 Coimbra, Portugal Kyushu Univ, Inst Adv Mat Study, Fukuoka 8168580, Japan Kyushu Univ Fukuoka Japan 8168580 Adv Mat Study, Fukuoka 8168580, Japan Kyushu Univ, Grad Sch Engn, Fukuoka 8168580, Japan Kyushu Univ Fukuoka Japan 8168580 Grad Sch Engn, Fukuoka 8168580, Japan
Titolo Testata:
APPLIED RADIATION AND ISOTOPES
fascicolo: 2, volume: 54, anno: 2001,
pagine: 227 - 239
SICI:
0969-8043(200102)54:2<227:SABEOT>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
SITE-SELECTIVE METALATION; IODINE-123-LABELED Z-MIVE; TISSUE DISTRIBUTION; RECEPTOR-BINDING; BREAST-CANCER; 17-ALPHA-IODOVINYL-11-BETA-METHOXYESTRADIOL MIVE2; DERIVATIVES; RADIOLIGAND; CARCINOMA; LIGANDS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Physical, Chemical & Earth Sciences
Citazioni:
18
Recensione:
Indirizzi per estratti:
Indirizzo: Patricio, L Inst Tecnol & Nucl, Estrada Nacl 10, P-2685 Sacavem, Portugal Inst Tecnol & Nucl Estrada Nacl 10 Sacavem Portugal P-2685 al
Citazione:
M.C.M.E. Silva et al., "Synthesis and biological evaluation of two new radiolabelled estrogens: [I-125](E)-3-methoxy-17 alpha-iodovinylestra-1,3,5(10),6-tetraen-17 beta-ol and [I-125](Z)-3-methoxy-17 alpha-iodovinylestra-1,3,5(10),6-tetraen-17 beta-ol", APPL RAD IS, 54(2), 2001, pp. 227-239

Abstract

The synthesis of two novel radiolabelled estrogen derivatives, [I-125](E)-3-methoxy-17 alpha -iodovinylestra-1,3,5(10),6-tetraen-17 beta -ol (E[I-125]IVDE) and [I-125](Z)-3-methoxy-17 alpha -iodovinylestra-1,3,5(10),6-tetraen-17 beta -ol (Z[I-125]IVDE), was carried out aiming to study the influenceof the introduction of a C6-C7 double bond on the biological properties ofthe estradiol molecule. 3-Methoxyestra-1,3,5(10),6-tetraen-17-one was synthesised starting from a suitably protected estrone and subsequently converted into the 17 alpha -ethynyl derivative. The radioiodinated derivatives were stereoselectively formed by radioiododestannylation of the correspondingtributylstannyl precursors. The biodistribution of the novel [I-125]iodovinylestradiol derivatives was evaluated in immature female mice. Biological data indicated that the Z-isomer, owing to its higher in vivo uptake by thetarget tissue, has the preferable configuration for further development ofsimilar compounds for estrogen receptor detection. (C) 2000 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 18:29:42