Synthesis and evaluation of cis-1-[4-(Hydroxymethyl)-2-cyclopenten-1-yl]-5-[(124)I]iodouracil: A new potential PET Imaging agent for HSV1-tk expression
- Title
- Synthesis and evaluation of cis-1-[4-(Hydroxymethyl)-2-cyclopenten-1-yl]-5-[(124)I]iodouracil: A new potential PET Imaging agent for HSV1-tk expression
- Author
- 이학준
- Issue Date
- 2007-11
- Publisher
- American Chemical Society
- Citation
- Journal of Medicinal Chemistry, v. 50, NO. 24, Page. 6032-6038
- Abstract
- In our pursuit to find an appropriate reporter probe for herpes simplex virus type-1 thymidine kinase (HSV1-tk), a carbocyclic nucleoside analogue, cis-1-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-5-[1241] iodouracil, has been efficiently synthesized. A Pd(0)-catalyzed coupling reaction together with organotin and exchange reactions for radiolabeling gave more than 80% radiochemical yield with greater than 95% radiochemical purity and 1.15 GBq/mu mol specific activity. Biological data reveal that the analogue is stable in vitro, less toxic than ganciclovir (GCV), and selective to HSV1-tk-expressed cells based on micro positron emission tomography (microPET) image analyses. Thus, this new carbocyclic nucleoside, referred to in this paper as carbocyclic 2',3'-didehydro-2',3'-dideoxy-5-iodouridine (carbocyclic d41U) is a potential imaging probe for HSV1-tk.
- URI
- https://pubs.acs.org/doi/10.1021/jm070791ghttps://repository.hanyang.ac.kr/handle/20.500.11754/183993
- ISSN
- 0022-2623;1520-4804
- DOI
- 10.1021/jm070791g
- Appears in Collections:
- COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E](과학기술융합대학) > CHEMICAL AND MOLECULAR ENGINEERING(화학분자공학과) > Articles
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