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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
- Authors
- Ahn, Hyunseok; Choi, Tae Hyun; De Castro, Kathlia; Lee, Kyo Chu; Kim, Byoungsoo; Moon, Byung Seok; Hong, Su Hee; Lee, Jong Chan; Chun, Kwon Soo; Cheon, Gi Jeong; Lim, Sang Moo; An, Gwang Il; Rhee, Hakjune
- Issue Date
- Nov-2007
- Publisher
- American Chemical Society
- Citation
- Journal of Medicinal Chemistry, v.50, no.24, pp 6032 - 6038
- Pages
- 7
- Indexed
- SCIE
SCOPUS
- Journal Title
- Journal of Medicinal Chemistry
- Volume
- 50
- Number
- 24
- Start Page
- 6032
- End Page
- 6038
- ISSN
- 0022-2623
1520-4804
- 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.
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Related Researcher
- Rhee, Hak june
- ERICA 공학대학 (ERICA 에너지바이오학과)