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Four new classes of 11 beta-substituted estradiol and estriol derivatives (cyanoalkyl, ethynyl, propynyl, and iodovinyl) have been synthesized, and their binding affinity for the estrogen receptor has been evaluated. The binding affinity values indicate that the estrogen receptor has tolerance for estradiol derivatives bearing 11 beta-groups whose size, rigidity, and polarity are limited. The estradiol derivatives have higher affinity than the estriol derivatives. The potential of these agents as imaging agent for estrogen receptor-positive breast tumors is discussed. On the basis of the results of this and a previously reported study (Napolitano, E.; Fiaschi, R.; Carlson, K. E.; Katzenellenbogen, J. A. 11 beta-Substituted Estradiol Derivatives, Potential High-Affinity Carbon-11-Labeled Probes for the Estrogen Receptor: A Structure-Affinity Relationship Study. J. Med. Chem. 1995, 38, 429-434), a general strategy for designing high-affinity probes for the estrogen receptor is proposed.
E Napolitano, and
R Fiaschi, and
K E Carlson, and
J A Katzenellenbogen
January 1988,
Steroids,
E Napolitano, and
R Fiaschi, and
K E Carlson, and
J A Katzenellenbogen
April 1984,
Journal of medicinal chemistry,
E Napolitano, and
R Fiaschi, and
K E Carlson, and
J A Katzenellenbogen
February 1992,
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology,
E Napolitano, and
R Fiaschi, and
K E Carlson, and
J A Katzenellenbogen
September 1979,
Science (New York, N.Y.),
E Napolitano, and
R Fiaschi, and
K E Carlson, and
J A Katzenellenbogen
May 1990,
Steroids,
E Napolitano, and
R Fiaschi, and
K E Carlson, and
J A Katzenellenbogen
December 2008,
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine,
E Napolitano, and
R Fiaschi, and
K E Carlson, and
J A Katzenellenbogen
October 1987,
Journal of steroid biochemistry,
E Napolitano, and
R Fiaschi, and
K E Carlson, and
J A Katzenellenbogen
January 1983,
Biochimica et biophysica acta,
E Napolitano, and
R Fiaschi, and
K E Carlson, and
J A Katzenellenbogen
March 2006,
Steroids,
E Napolitano, and
R Fiaschi, and
K E Carlson, and
J A Katzenellenbogen
April 2008,
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine,
