David G. Calatayud - Applications of "Hot" and "Cold" Bis(thiosemicarbazonato) Metal Complexes in Multimodal Imaging

Version 1

      Publication Details (including relevant citation   information):

      Cortezon-Tamarit, F., Sarpaki, S., Calatayud, D.G., Mirabello,   V., Pascu, S.I. Chemical Record 2016  1380-1397

      Abstract: © 2016 The Chemical Society of Japan   & Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.The   applications of coordination chemistry to molecular imaging has   become a matter of intense research over the past 10 years. In   particular, the applications of bis(thiosemicarbazonato) metal   complexes in molecular imaging have mainly been focused on   compounds with aliphatic backbones due to the in vivo imaging   success of hypoxic tumors with PET (positron emission tomography)   using 64CuATSM [copper   (diacetyl-bis(N4-methylthiosemicarbazone))]. This compound   entered clinical trials in the US and the UK during the first   decade of the 21st century for imaging hypoxia in head and neck   tumors. The replacement of the ligand backbone to aromatic   groups, coupled with the exocyclic N's functionalization during   the synthesis of bis(thiosemicarbazones) opens the possibility to   use the corresponding metal complexes as multimodal imaging   agents of use, both in vitro for optical detection, and in vivo   when radiolabeled with several different metallic species. The   greater kinetic stability of acenaphthenequinone   bis(thiosemicarbazonato) metal complexes, with respect to that of   the corresponding aliphatic ATSM complexes, allows the   stabilization of a number of imaging probes, with special   interest in "cold" and "hot" Cu(II) and Ga(III) derivatives for   PET applications and 111In(III) derivatives for SPECT   (single-photon emission computed tomography) applications, whilst   Zn(II) derivatives display optical imaging properties in cells,   with enhanced fluorescence emission and lifetime with respect to   the free ligands. Preliminary studies have shown that   gallium-based acenaphthenequinone bis(thiosemicarbazonato)   complexes are also hypoxia selective in vitro, thus increasing   the interest in them as new generation imaging agents for in   vitro and in vivo applications.

      Address (URL):