Synthesis and biological evaluation of [18F] bicalutamide, 4-[76Br] bromobicalutamide, and 4-[76Br] bromo-thiobicalutamide as non-steroidal androgens for prostate …

EE Parent, CS Dence, C Jenks, TL Sharp…

文献索引：Parent, Ephraim E.; Dence, Carmen S.; Jenks, Carl; Sharp, Terry L.; Welch, Michael J.; Katzenellenbogen, John A. Journal of Medicinal Chemistry, 2007 , vol. 50, # 5 p. 1028 - 1040

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被引用次数: 30

摘要

Androgen receptors (AR) are overexpressed in most primary and metastatic prostate cancers. To develop a nonsteroidal AR-mediated imaging agent, we synthesized and radiolabeled several analogs of the potent antiandrogen bicalutamide:[18F] bicalutamide, 4- [76Br] bromobicalutamide, and [76Br] bromo-thiobicalutamide. Two of these analogs, 4- [76Br] bromobicalutamide and [76Br] bromo-thiobicalutamide, were found to have a ...