Synthesis and binding affinities of novel Re-containing 7α-substituted estradiol complexes: models for breast cancer imaging agents

…, FR Wüst, JA Katzenellenbogen

Index: Skaddan, Marc B.; Wuest, Frank R.; Katzenellenbogen, John A. Journal of Organic Chemistry, 1999 , vol. 64, # 22 p. 8108 - 8121

Full Text: HTML

Citation Number: 95

Abstract

The diagnosis and staging of breast cancer could be improved by the development of imaging radiopharmaceuticals that provide a noninvasive determination of the estrogen receptor status in the tumor cells. Toward this goal, we have synthesized a number of novel Re-containing 7α-substituted estradiol complexes. The introduction of the 7α side chain involves the alkylation of tetrahydropyranyloxy-protected 6-keto estradiol. The methods ...