TY - JOUR
T1 - The synthesis of non-steroidal estrogen receptor binding compounds labeled with 80mBr
AU - Seevers, R. H.
AU - Mease, R. C.
AU - Friedman, A. M.
AU - Desombre, E. R.
N1 - Funding Information:
Acknowledgements-We would like to thank Dr 0. T. DeJesus of the Department of Radiology, The University of Chicago, for his helpful discussions. We would also like to thank Michael J. Wendel and Tina M. Wator, both par-ticiptants in the Student Research Participation Program coordinated by the Division of Education Programs, Argonne National Laboratory, for their assistance in the synthetic portion of this work. This work was supported in part by a grant from the NC1 [CA-274761.
PY - 1986
Y1 - 1986
N2 - Estrogen receptor (ER) binding radiopharmaceuticals have potenial for use in the diagnosis and treatment of cancers of the female reproductive system. Two triphenylethylene derivatives based on the structure of hydroxytamoxifen 4, a high ER binding metabolite of tamoxifen 5, have been prepared: 1-(4-dimethylaminoethoxy)phenyl]-1-(4-hydroxy)phenyl-2-bromo-2-phenylethylene 2 and 1,1-bis(p-hydroxyphenyl)-2-bromo-2-phenylethylene 3. Both 2 and 3 bind strongly to the ER. Compound 3 has been labeled in modest yield by direct bromination with 80mBr, which was produced by the 83Kr (d,nα) reaction. Radiolabeled 22, a dimethoxy precursor of 3, has been prepared in yields ranging between 40 and 60% by a bromination destannylation reaction.
AB - Estrogen receptor (ER) binding radiopharmaceuticals have potenial for use in the diagnosis and treatment of cancers of the female reproductive system. Two triphenylethylene derivatives based on the structure of hydroxytamoxifen 4, a high ER binding metabolite of tamoxifen 5, have been prepared: 1-(4-dimethylaminoethoxy)phenyl]-1-(4-hydroxy)phenyl-2-bromo-2-phenylethylene 2 and 1,1-bis(p-hydroxyphenyl)-2-bromo-2-phenylethylene 3. Both 2 and 3 bind strongly to the ER. Compound 3 has been labeled in modest yield by direct bromination with 80mBr, which was produced by the 83Kr (d,nα) reaction. Radiolabeled 22, a dimethoxy precursor of 3, has been prepared in yields ranging between 40 and 60% by a bromination destannylation reaction.
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U2 - 10.1016/0883-2897(86)90029-2
DO - 10.1016/0883-2897(86)90029-2
M3 - Article
C2 - 3793506
AN - SCOPUS:0022443632
SN - 0969-8051
VL - 13
SP - 483
EP - 495
JO - International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
JF - International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
IS - 4
ER -