Bromine-and iodine-substituted 16α, 17α-dioxolane progestins for breast tumor imaging and radiotherapy: synthesis and receptor binding affinity

…, KE Carlson, JA Katzenellenbogen…

Index: Zhou, Dong; Carlson, Kathryn E.; Katzenellenbogen, John A.; Welch, Michael J. Journal of Medicinal Chemistry, 2006 , vol. 49, # 15 p. 4737 - 4744

Full Text: HTML

Citation Number: 22

Abstract

Progesterone receptors (PRs) are present in many breast tumors, and their levels are increased by certain endocrine therapies. We describe the synthesis and PR binding affinities of a series of bromine-and iodine-substituted 16α, 17α-dioxolane progestins, some of which, when appropriately radiolabeled, are potential agents for diagnostic imaging of PR- positive breast tumors using positron emission tomography (PET) and for radiotherapy. ...