RESUMEN
This paper describes recent studies in organic sonoelectrochemistry at Coventry University, including the oxidation of thiophene monoxides, degradation of dye pollutants, formation of conducting polymers and electrosynthetic modification of proteins.
Asunto(s)
Química Orgánica/métodos , Electroquímica/métodos , Ultrasonido , Animales , Compuestos Azo/química , Colorantes/química , Humanos , Oxidación-Reducción , Polímeros/química , Proteínas/química , Tiofenos/químicaRESUMEN
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.
Asunto(s)
Congéneres del Estradiol/síntesis química , Congéneres del Estradiol/farmacocinética , Estradiol/análogos & derivados , Estradiol/síntesis química , Estradiol/farmacocinética , Animales , Neoplasias de la Mama/diagnóstico por imagen , Neoplasias de la Mama/metabolismo , Femenino , Humanos , Radioisótopos de Yodo , Ratones , Cintigrafía , Receptores de Estrógenos/metabolismo , Estereoisomerismo , Distribución Tisular , Útero/metabolismoRESUMEN
In the title compound, pentacyclo[11.8.1.1(3,11).0(7,23).0(15, 20)]tricosa-3,5,7,9,11(23),15,17,19-octaen-22-one, C(23)H(20)O, the bicyclo[5.4.1]dodecan-12-one moiety takes a rigid conformation in which the seven- and eight-membered rings take chair and boat-boat forms, respectively. The molecule has a non-crystallographic mirror symmetry perpendicular to the benzene and naphthalene planes.
