High affinity tamoxifen derivatives and uses thereof

Details High affinity tamoxifen derivatives and uses thereof High affinity tamoxifen derivatives and uses thereof

1991-06-28

1993-03-09

Stoll, Robert L.

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

128659, A61K 4902, A61K 4300

Patent

active

051925257

ABSTRACT:
The synthesis of tamoxifen derivatives, most particularly halo, haloalkyl and hydroxy tamoxifen derivatives, wherein the native tamoxifen molecule includes a substituted chemical group positioned on the aliphatic chain of the tamoxifen molecule, is provided. Methods for imaging estrogen receptors using the tamoxifen derivatives of the invention are also described. The aliphatic chain substituted tamoxifen derivatives of the invention possess greater estrogen receptor binding affinities and more potent tumor cell inhibiting activity than native tamoxifen or tamoxifen derivatives substituted at other locations on the molecule (i.e., non-aliphatic chain substituted tamoxifen, phenolic-ring substituted tamoxifen). Examples of the halogenated tamoxifen derivatives of the invention include chloro-, bromo-, iodo- and fluoro-tamoxifen derivatives, and their corresponding lower alkyl halogenated forms.

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