Synthesis and in vitro receptor binding studies of fluorotamoxifen analogues

We describe the synthesis of new fluorotamoxifen analogues with the fluorine atom positioned on the end of the aliphatic chain of tamoxifen. The binding of fluorotamoxifens to cytosol estrogen receptors of rat uteri was determined with [3H]estradiol (5 nM). The fluorotamoxifens had similar or superi...

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Veröffentlicht in:Pharmaceutical research 1991-02, Vol.8 (2), p.174-177
Hauptverfasser: YANG, D. J, WALLACE, S, TANSEY, W, WRIGHT, K. C, LI-REN KUANG, TILBURY, R. S, DIEGO, I, LIM, J.-L, EMRAN, A. M, KIM, E. E
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Sprache:eng
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Zusammenfassung:We describe the synthesis of new fluorotamoxifen analogues with the fluorine atom positioned on the end of the aliphatic chain of tamoxifen. The binding of fluorotamoxifens to cytosol estrogen receptors of rat uteri was determined with [3H]estradiol (5 nM). The fluorotamoxifens had similar or superior binding affinities compared with tamoxifen. The IC50 value was as follows: tamoxifen, 5 x 10(-7) M; fluorotamoxifen (VII), 5 x 10(-7) M; N,N-diethylfluorotamoxifen (IV)-cis, 1 x 10(-6) M, and trans, 2 x 10(-7) M; and (cis) fluoromethyl-N,N-diethyltamoxifen (VI) 1 x 10(-7) M. Therefore, the fluorinated tamoxifens have potential use in imaging estrogen receptors by PET.
ISSN:0724-8741
1573-904X
DOI:10.1023/A:1015879717742