Synthesis and biological evaluation of two new radiolabelled estrogens: [125I](E)-3-methoxy-17alpha-iodovinylestra-1,3,5(10),6-tetraen-17beta-ol and

Autor:	M C, Melo e Silva, L, Patrćio, L, Gano, M L, Sá e Melo, E, Inohae, S, Mataka, T, Thiemann
Rok vydání:	2001
Předmět:	Iodine Radioisotopes Mice Estradiol Estradiol Congeners Receptors Estrogen Uterus Animals Humans Breast Neoplasms Female Stereoisomerism Tissue Distribution Radionuclide Imaging
Zdroj:	Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine. 54(2)
ISSN:	0969-8043
Popis:	The synthesis of two novel radiolabelled estrogen derivatives, [125I](E)-3-methoxy-17alpha-iodovinylestra-1,3,5(10),6-tetraen-17beta-ol (E[125I]IVDE) and [125I](Z)-3-methoxy-17alpha-iodovinylestra-1,3,5(10),6-tetraen-17beta-ol (Z[125I]IVDE), was carried out aiming to study the influence of the introduction of a C6-C7 double bond on the biological properties of the 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 17alpha-ethynyl derivative. The radioiodinated derivatives were stereoselectively formed by radioiododestannylation of the corresponding tributylstannyl precursors. The biodistribution of the novel [125I]iodovinylestradiol derivatives was evaluated in immature female mice. Biological data indicated that the Z-isomer, owing to its higher in vivo uptake by the target tissue, has the preferable configuration for further development of similar compounds for estrogen receptor detection.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::e2ec3a2e22d615e02b053ddd1753df77 https://pubmed.ncbi.nlm.nih.gov/11200884 Zobrazit plný text záznamu Full Text from ScienceDirect