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Synthesis and biological evaluation of 99m Tc(CO) 3 (IDA‐CPT) for tumor imaging
Author(s) -
Wang Jianjun,
Niu Tingting,
Yang Jing,
Tan Cunmin,
Zheng Xiaobei,
Wu Wangsuo,
Dong Feng,
Guo Hongyun
Publication year - 2009
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1690
Subject(s) - biodistribution , chemistry , iminodiacetic acid , linker , camptothecin , in vivo , radiochemistry , methylene , yield (engineering) , norvaline , chelation , stereochemistry , nuclear chemistry , in vitro , medicinal chemistry , biochemistry , organic chemistry , amino acid , materials science , microbiology and biotechnology , computer science , metallurgy , biology , operating system , leucine
This work reports the synthesis, radiolabeling, and preliminary biodistribution results in tumor‐bearing mice of 99m Tc(CO) 3 (IDA‐CPT). The novel camptothecin (CPT) derivate was successfully synthesized by conjugation of iminodiacetic acid (IDA) to camptothecin via a short carbonyl‐methylene linker. Radiolabeling was performed in high yield with [ 99m Tc(CO) 3 ] + core to get 99m Tc(CO) 3 (IDA‐CPT), which was hydrophilic and stable at room temperature. Biodistribution studies in tumor‐bearing mice showed that 99m Tc(CO) 3 (IDA‐CPT) accumulated in the tumor with good uptake and retention. However, its clearance from normal organs was slow, resulting in poor T/NT ratios. Further modification on the linker or/and 99m Tc‐chelate to improve the tumor‐targeting efficacy and in vivo kinetic profiles is currently in progress. Copyright © 2009 John Wiley & Sons, Ltd.