ISSN:
1573-904X
Keywords:
estrogen
;
receptor
;
fluorotamoxifen
;
synthesis
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract 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 × 10−7 M; fluorotamoxifen (VII), 5 × 10−7 M; N,N-diethylfluorotamoxifen (IV)—cis, 1 × 10−6 M, and trans, 2 × 10−7 M; and (cis) fluoromethyl-N,N-diethyltamoxifen (VI) 1 × 10−7 M. Therefore, the fluorinated tamoxifens have potential use in imaging estrogen receptors by PET.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1023/A:1015879717742
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