Abstract
The synthesis of two novel radiolabelled estrogen derivatives, [ 125I]( E)-3-methoxy-17 α-iodovinylestra-1,3,5(10),6-tetraen-17 β-ol ( E[ 125I]IVDE ) and [ 125I]( Z)-3-methoxy-17 α-iodovinylestra-1,3,5(10),6-tetraen-17 β-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 17 α-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.
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