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Aminoferrocene‐Based Anticancer Prodrugs Labelled with Cyanine Dyes for in vivo Imaging
Author(s) -
Gizem Özkan Hülya,
Toms Johannes,
Maschauer Simone,
Prante Olaf,
Mokhir Andriy
Publication year - 2021
Publication title -
european journal of inorganic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.667
H-Index - 136
eISSN - 1099-0682
pISSN - 1434-1948
DOI - 10.1002/ejic.202100829
Subject(s) - prodrug , chemistry , biodistribution , cyanine , in vivo , conjugate , preclinical imaging , positron emission tomography , in vitro , reactive oxygen species , fluorescence , biophysics , biochemistry , nuclear medicine , medicine , mathematical analysis , physics , microbiology and biotechnology , mathematics , quantum mechanics , biology
N‐alkylaminoferrocene‐based (NAAF) prodrugs are activated in the presence of reactive oxygen species (ROS), based on which these prodrugs target cancer cells (high ROS) and do not affect normal cells (low ROS). To gain some insights into their mode of action in vivo, we have investigated the biodistribution of 18 F‐labelled NAAF prodrugs in tumor‐bearing mice by positron emission tomography (PET). Due to the short half‐life of 18 F, the experimental time frame was restricted to 60 min. To extend the observation window, a more stable marker is required. In this paper, we report on conjugates of NAAF prodrugs with two cyanine dyes Cy5 and Cy7 including details of their synthesis, characterization and basic properties in cell free settings and their cellular uptake in representative human cancer cells. Finally, the Cy5 conjugate was subjected to in vivo fluorescence imaging studies to determine the prodrug biodistribution over 24 h.