@article{oai:repo.qst.go.jp:00084559,
 author = {Suzuki, Hiroyuki (Chiba Univ.) and Kaizuka,, Yuta (Chiba Univ.) and Tatsuta,, Maho (Tokyo Inst. Tech.) and Tanaka, Hiroshi (Tokyo Inst. Tech.) and Washiya,, Nana (Chiba Univ.) and Shirakami,, Yoshifumi (Osaka Univ.) and Ooe,, Kazuhiro (Osaka Univ.) and Toyoshima,, Atsushi (Osaka Univ.) and Watabe,, Tadashi (Osaka Univ.) and Teramoto,, Takahiro (Osaka Univ.) and Ichiro, Sasaki and Shigeki, Watanabe and Noriko, Ishioka and Hatazawa,, Jun (Osaka Univ.) and Uehara,, Tomoya (Chiba Univ.) and Arano,, Yasushi (Chiba Univ.) and Hiroyuki, Suzuki and Hiroshi, Tanaka and Ichiro, Sasaki and Shigeki, Watanabe and Noriko, Ishioka},
 issue = {21},
 journal = {Journal of Medicinal Chemistry},
 month = {Nov},
 note = {The high in vivo stability of 2,2-dihydroxymethyl-3-[18F]fluoropropyl-2-nitroimidazole ([18F]DiFA) prompted us to evaluate neopentyl as a scaffold to prepare a radiotheranostic system with radioiodine and astatine.Three DiFA derivatives with one, two, or without a hydroxyl group were synthesized. While all 125I-labeled compounds remained stable against nucleophilic substitution, only a 125I-labeled neopentyl glycol was stable against cytochrome P450 (CYP)-mediated metabolism and showed high stability against in vivo deiodination. 211At-labeled neopentyl glycol also remained stable against both nucleophilic substitution and CYP-mediated metabolism. 211At labeled neopentyl glycol showed the biodistribution profiles similar to those of its radioiodinated counterpart in contrast to the 125I/211At-labeled benzoate pair. The urine analyses confirmed that 211At-labeled neopentyl glycol was excreted in the urine as a glucuronide conjugate with the absence of free [211At]At-. These findings indicate that neopentyl glycol would constitute a promising scaffold to prepare a radiotheranostic system with radioiodine and 211At.},
 pages = {15846--15857},
 title = {Neopentyl glycol as a scaffold to provide radiohalogenated theranostic pairs of high in vivo stability},
 volume = {64},
 year = {2021}
}