05192525 is referenced by 55 patents and cites 5 patents.

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.

Title
High affinity tamoxifen derivatives and uses thereof
Application Number
589928
Publication Number
5192525
Application Date
June 28, 1991
Publication Date
March 9, 1993
Inventor
Sidney Wallace
Houston
TX, US
David J Yang
Sugarland
TX, US
Agent
Arnold White & Durkee
Assignee
Board of Regents The University of Texas System
TX, US
IPC
A61K 43/00
A61K 49/02
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