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http://dx.doi.org/10.5012/bkcs.2008.29.3.595

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)
Publication Information
Bulletin of the Korean Chemical Society / v.29, no.3, 2008 , pp. 595-598 More about this Journal
Abstract
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.
Keywords
Emodin; 2-[123I]iodoemodin; HER-2/neu; Breast cancer; Tumor imaging
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