Nuclear Medicine and Molecular Imaging
- Volume 43 Issue 5
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- Pages.478-486
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- 2009
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- 1869-3474(pISSN)
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- 1869-3482(eISSN)
The Synthesis of the Stable IVDU Derivative for Imaging HSV-1 TK Expression
체내 안정형 HSV1-tk (Herpes Simplex Virus Type-1 Thymidine Kinase) 영상용 IVDU 유도체의 합성
- Kim, Eun-Jung (Laboratory of Radiopharmaceutical Research, Korea Institute of Radiological and Medical Science (KIRAMS)) ;
- Choi, Tae-Hyun (Laboratory of Radiopharmaceutical Research, Korea Institute of Radiological and Medical Science (KIRAMS)) ;
- Ahn, Soon-Hyuk (Laboratory of Radiopharmaceutical Research, Korea Institute of Radiological and Medical Science (KIRAMS)) ;
- Kim, Byoung-Soo (Laboratory of Radiopharmaceutical Research, Korea Institute of Radiological and Medical Science (KIRAMS)) ;
- Park, Hyun (Laboratory of Radiopharmaceutical Research, Korea Institute of Radiological and Medical Science (KIRAMS)) ;
- Cheon, Gi-Jeong (Laboratory of Radiopharmaceutical Research, Korea Institute of Radiological and Medical Science (KIRAMS)) ;
- Rhee, Hak-June (Department of Chemistry and Applied Chemistry, Hanyang University) ;
- An, Gwang-Il (Laboratory of Radiopharmaceutical Research, Korea Institute of Radiological and Medical Science (KIRAMS))
- 김은정 (한국원자력의학원 방사성의약품연구팀) ;
- 최태현 (한국원자력의학원 방사성의약품연구팀) ;
- 안순혁 (한국원자력의학원 방사성의약품연구팀) ;
- 김병수 (한국원자력의학원 방사성의약품연구팀) ;
- 박현 (한국원자력의학원 방사성의약품연구팀) ;
- 천기정 (한국원자력의학원 방사성의약품연구팀) ;
- 이학준 (한양대학교 응용화학과) ;
- 안광일 (한국원자력의학원 방사성의약품연구팀)
- Published : 2009.10.31
Abstract
Purpose: 5-iododeoxyuridine analogues have been exclusively developed for the potential antiviral and antitumor therapeutic agents. In this study, we synthesized carbocyclic radioiododeoxyuridineanalogue (ddIVDU) and carbocyclic intermediate as efficient carbocyclic radiopharmaceuticals. Materials and Methods: The synthesis is LAH reduction, hetero Diels-Alder reaction as key reactions including Pd(0)-catalyzed coupling reaction together with organotin. MCA-RH7777 (MCA) and MCA-tk (HSV1-tk positive) cells were treated with various concentration of carbocyclic ddIVDU, and GCV. Cytotoxicity was measured by the MTS methods. For in vitro uptake study, MCA and MCA-tk cells were incubated with 1uCi of [
목적: 화합물이 가지는 항바이러스 및 항암 작용으로 인하여 5-iododeoxyuridine 유도체들에 관한 연구는 매우 광범위하게 이루어져왔다. 방사 요오드가 치환된 이들 화합물에 대한 연구의 주요 목표는 체내 및 체외 평가 시 효과적 일뿐만 아니라, 보다 안정한 화합물을 개발하는 것이다. 본 연구를 통해, 다양한 방사성의약품의 중간체로도 이용되어질 수 있는 carbocyclic radioiododeoxyuridineanalogue (ddIVDU)를 합성하여 생물학적 평가를 수행하고자 하였다. 대상 및 방법: 목표 화합물의 합성은 Pd(0)-촉매 결합 반응, LAH 환원반응, hetero Diels-Alder 반응을 주요 반응으로 하여 수행하였다