Synthesis of 7alpha-substituted derivatives of 17beta-estradiol.
@article{Jiang2006SynthesisO7, title={Synthesis of 7alpha-substituted derivatives of 17beta-estradiol.}, author={Xiang-Rong Jiang and J. W. Sowell and B. Zhu}, journal={Steroids}, year={2006}, volume={71 5}, pages={ 334-42 } }
Estrogen receptor (ER) pure antagonists such as ICI-182,780 (fulvestrant) are effective alternatives to tamoxifen (an ER antagonist/weak partial agonist) in the treatment of postmenopausal, receptor-positive human breast cancers. Structurally, these pure antagonists contain the basic core structure of 17beta-estradiol (E(2)) with a long side chain attached to its C-7alpha position. We explored and compared in this study various synthetic routes for preparing a number of C-7alpha-substituted… CONTINUE READING