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Ester derivatives of the mammary-tumor-inhibiting antiestrogen 2,3-bis(2-fluoro-4-hydroxyphenyl)-2,3-dimethylbutane

Schwarz, W. ; Hartmann, R. W. ; Engel, J. ; Schneider, M. R. ; Schönenberger, Helmut


The synthesis of the bisacetate (8), the bisdichloroacetate (9), the biscarbamate (10) and the bisphosphate (11) of the "partial" antiestrogen 2,3-bis(2-fluoro-4-hydroxyphenyl)-2,3-dimethylbutane (7) is described. In the case of 8-10 the introduction of ester functions slightly reduces the estrogen receptor affinity of 7. However, it was strongly diminished in 11. Compared with 7 the estrogenic ...


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