Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada T6G 2N8.
Bioorg Med Chem Lett. 2011 Feb 15;21(4):1195-8. doi: 10.1016/j.bmcl.2010.12.091. Epub 2010 Dec 23.
A group of (Z)-1,2-diphenyl-1-[4-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl]but-1-enes were synthesized using methodologies that will allow incorporation of a [(124)I]iodine substituent at the para-position of either the C-1 phenyl ring or the C-2 phenyl ring, or a [(18)F]OCH(2)CH(2)F substituent at the para-position of the C-2 phenyl ring. These [(124)I] and [(18)F] radiotracers are designed as potential radiopharmaceuticals to image estrogen positive breast tumors using positron emission tomography (PET).
一组(Z)-1,2-二苯基-1-[4-[2-(4-甲基哌嗪-1-基)乙氧基]苯基]丁-1-烯通过将 [(124)I] 碘取代基引入 C-1 苯基环或 C-2 苯基环的对位,或者将 [(18)F]OCH(2)CH(2)F 取代基引入 C-2 苯基环的对位的方法合成。这些 [(124)I] 和 [(18)F] 放射性示踪剂被设计为潜在的放射性药物,用于使用正电子发射断层扫描(PET)成像雌激素阳性乳腺癌肿瘤。