Halogenated analogues of tamoxifen: Synthesis, receptor assay, and inhibition of MCF7 cells

…, G Reger, A Cherif, KC Wright, R Moult…

Index: Yang; Tewson; Tansey; Kuang; Reger; Cherif; Wright; Moult; Tilbury; Chu; Kim; Wallace Journal of Pharmaceutical Sciences, 1992 ,  vol. 81,  # 7  p. 622 - 625

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Citation Number: 24

Abstract

Abstract This study was conducted to develop a ligand for imaging estrogen-receptor- positive breast tumors by positron emission tomography or single photon emission computed tomography. We synthesized fluoro and iodo analogues of tamoxifen, and these halogenated analogues produced greater affinity for binding to the receptor than tamoxifen. Values of the inhibition affinity constants were as follows: tamoxifen, 15 000 nM; ...