Triaryl (Z)-olefins suitable for radiolabeling with iodine-124 or fluorine-18 radionuclides for positron emission tomography imaging of estrogen positive breast tumors

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1195-8. doi: 10.1016/j.bmcl.2010.12.091. Epub 2010 Dec 23.

Abstract

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).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemical synthesis
  • Alkenes / chemistry*
  • Breast Neoplasms / diagnosis*
  • Female
  • Fluorine Radioisotopes / chemistry
  • Humans
  • Iodine Radioisotopes / chemistry
  • Isotope Labeling
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / chemistry*
  • Receptors, Estrogen / metabolism

Substances

  • Alkenes
  • Fluorine Radioisotopes
  • Iodine Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Estrogen