Bulletin of the Korean Chemical Society

  • 제29권3호
  • /
  • Pages.595-598
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  • 2008
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  • 0253-2964(pISSN)
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  • 1229-5949(eISSN)
대한화학회 (Korean Chemical Society)
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Synthesis and Evaluation of 2-[123I]iodoemodin for a Potential Breast Cancer Imaging Agent

  • Park, Jeong-Hoon (Department of Chemistry, Dongguk University) ;
  • Kim, Sang-Wook (Radiation Research Center for Industry & Environment, Korea Atomic Energy Research Institute) ;
  • Yang, Seung-Dae (Radiation Research Center for Industry & Environment, Korea Atomic Energy Research Institute) ;
  • Hur, Min-Goo (Radiation Research Center for Industry & Environment, Korea Atomic Energy Research Institute) ;
  • Chun, Kwon-Soo (Cyclotron Application Laboratory, Korea Cancer Center Hospital) ;
  • Yu, Kook-Hyun (Department of Chemistry, Dongguk University)
  • 발행 : 2008.03.20
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초록

Emodin (3-methyl-1,6,8-trihydroxyanthraquinone) is a natural chemotherapeutic compound with diverse biological properties including an antitumor activity. Emodin, a specific inhibitor of the protein tyrosine kinase, has a number of cellular targets in related to it. Its inhibition activity affects the mammalian cell cycle regulation in specific oncogene. Practically, it has been proven to inhibit HER-2/neu tyrosine kinase expressing breast cancer cells as an anticancer agent. 2-[123I]iodoemodin has been synthesized and evaluated human breast cancer cells (MDA-MB-231, MCF-7, fibroblast as a control) which express basal levels of HER-2/neu tyrosine kinase to investigate its suitability as a breast cancer imaging agent and 2-iodoemodin has been synthesized as a standard compound. The radiochemical yield of the 2-[123I]iodoemodin was about 72% and its radiochemical purity was over 97% after purification. The radioactivity of the 2-[123I]iodoemodin was increased in a time dependent manner in both cell lines and the ratio of MDA-MB-231 and MCF7 to fibroblast was 2.9 and 1.7, respectively.

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