synthesis, radiolabeling and biological evaluation of propylene amine oxime complexes containing nitrotriazoles as hypoxia markers合成、放射性标记和生物评价丙烯胺肟复合物含有nitrotriazoles缺氧标记.pdfVIP

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synthesis, radiolabeling and biological evaluation of propylene amine oxime complexes containing nitrotriazoles as hypoxia markers合成、放射性标记和生物评价丙烯胺肟复合物含有nitrotriazoles缺氧标记.pdf

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synthesis, radiolabeling and biological evaluation of propylene amine oxime complexes containing nitrotriazoles as hypoxia markers合成、放射性标记和生物评价丙烯胺肟复合物含有nitrotriazoles缺氧标记

Molecules 2012, 17, 6808-6820; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis, Radiolabeling and Biological Evaluation of Propylene Amine Oxime Complexes Containing Nitrotriazoles as Hypoxia Markers Huafan Huang, Lei Mei and Taiwei Chu * Beijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China * Author to whom correspondence should be addressed; E-Mail: twchu@; Tel./Fax: +86-10-6275-4319. Received: 10 May 2012; in revised form: 28 May 2012 / Accepted: 29 May 2012 / Published: 4 June 2012 Abstract: Two propylene amine oxime (PnAO) complexes, 1, containing a 3-nitro-1,2,4- triazole and 2, containing two 3-nitro-1,2,4-triazoles, were synthesized and radiolabeled with 99mTc in high labeling yields. Cellular uptakes of 99mTc-1 and 99mTc-2 were tested using a S180 cells line. Under anoxic conditions, the cellular uptakes of 99mTc-1 and 99mTc-2 were 33.7 ± 0.2% and 35.0 ± 0.7% at 4 h, whereas the normoxic uptakes of the two complexes were 6.0 ± 1.6% and 4.6 ± 0.9%, respectively. Both 99mTc-1 and 99mTc-2 displayed significant anoxic/normoxic differentials. The cellular uptakes were highly 99m dependen