TY  - JOUR
AU  - Kopp, Ina
AU  - Cieslik, Patrick
AU  - Anger, Karl
AU  - Josephy, Thomas
AU  - Neupert, Lucca
AU  - Velmurugan, Gunasekaran
AU  - Gast, Michael
AU  - Wadepohl, Hubert
AU  - Brühlmann, Santiago Andrés
AU  - Walther, Martin
AU  - Kopka, Klaus
AU  - Bachmann, Michael
AU  - Stephan, Holger
AU  - Kubeil, Manja
AU  - Comba, Peter
TI  - Bispidine Chelators for Radiopharmaceutical Applications with Lanthanide, Actinide, and Main Group Metal Ions.
JO  - Inorganic chemistry
VL  - 62
IS  - 50
SN  - 0020-1669
CY  - Washington, DC
PB  - American Chemical Society
M1  - DKFZ-2023-01877
SP  - 20754-20768
PY  - 2023
N1  - 2023 Dec 18;62(50):20754-20768
AB  - Octadentate and specifically nonadentate ligands with a bispidine scaffold (3,7-diazabicyclo[3.3.1]nonane) are known to be efficiently coordinated to a range of metal ions of interest in radiopharmaceutical chemistry and lead to exceedingly stable and inert complexes. Nonadentate bispidine L2 (with a tridentate bipyridine acetate appended to N3 and a picolinate at N7) has been shown before to be an ideal chelator for 111In3+, 177Lu3+, and 225Ac3+, nuclides of interest for diagnosis and therapy, and a proof-of-principle study with an SSTR2-specific octreotate has shown potential for theranostic applications. We now have extended these studies in two directions. First, we present ligand derivative L3, in which the bipyridine acetate is substituted with terpyridine, a softer donor for metal ions with a preference for more covalency. L3 did not fulfill the hopes because complexation is much less efficient. While for Bi3+ and Pb2+ the ligand is an excellent chelator with properties similar to those of L2, Lu3+ and La3+ show very slow and inefficient complexation with L3 in contrast to L2, and 225Ac3+ is not fully coordinated, even at an increased temperature (92
LB  - PUB:(DE-HGF)16
C6  - pmid:37707798
DO  - DOI:10.1021/acs.inorgchem.3c02340
UR  - https://inrepo02.dkfz.de/record/282875
ER  -