210366-15-7Relevant articles and documents
Alternative chelator for 89Zr radiopharmaceuticals: Radiolabeling and evaluation of 3,4,3-(LI-1,2-HOPO)
Deri, Melissa A.,Ponnala, Shashikanth,Zeglis, Brian M.,Pohl, Gabor,Dannenberg,Lewis, Jason S.,Francesconi, Lynn C.
, p. 4849 - 4860 (2014)
Zirconium-89 is an effective radionuclide for antibody-based positron emission tomography (PET) imaging because its physical half-life (78.41 h) matches the biological half-life of IgG antibodies. Desferrioxamine (DFO) is currently the preferred chelator for 89Zr4+; however, accumulation of 89Zr in the bones of mice suggests that 89Zr4+ is released from DFO in vivo. An improved chelator for 89Zr4+ could eliminate the release of osteophilic 89Zr4+ and lead to a safer PET tracer with reduced background radiation dose. Herein, we present an octadentate chelator 3,4,3-(LI-1,2-HOPO) (or HOPO) as a potentially superior alternative to DFO. The HOPO ligand formed a 1:1 Zr-HOPO complex that was evaluated experimentally and theoretically. The stability of 89Zr-HOPO matched or surpassed that of 89Zr-DFO in every experiment. In healthy mice, 89Zr-HOPO cleared the body rapidly with no signs of demetalation. Ultimately, HOPO has the potential to replace DFO as the chelator of choice for 89Zr-based PET imaging agents.
Synthesis and iron chelating properties of hydroxypyridinone and hydroxypyranone hexadentate ligands
Zhou, Tao,Kong, Xiao-Le,Hider, Robert C.
, p. 3459 - 3466 (2019/03/13)
Chelation therapy has become an important therapeutic approach for some diseases. In attempt to identify clinically useful chelators, four hexadentate ligands were synthesized by conjugating the corresponding bidentate ligands (3-hydroxypyridin-4-one (3,4-HOPO), 3-hydroxypyridin-2-one (3,2-HOPO), 1-hydroxypyridin-2-one (1,2-HOPO), and 3-hydroxypyran-4-one) each with a free amino group to a tripodal acid. Their pKa values and affinities for iron(iii) were investigated. The pFe3+ values of the hexadentate pyridinones 1 (3,4-HOPO), 3 (3,2-HOPO) and 4 (1,2-HOPO), and the pyranone 2 was found to follow the sequence 1 > 4 ? 3 > 2, which is different to the pFe3+ value sequence of the corresponding bidentate forms (3,4-HOPO ? 3,2-HOPO > 1,2-HOPO > 3-hydroxypyranone). Hexadentate 3,4-HOPOs and 1,2-HOPOs have the greatest potential as iron scavenging agents.
New insights into structure and luminescence of EuIII and SmIII complexes of the 3,4,3-LI(1,2-HOPO) ligand
Daumann, Lena J.,Tatum, David S.,Snyder, Benjamin E. R.,Ni, Chengbao,Law, Ga-Lai,Solomon, Edward I.,Raymond, Kenneth N.
supporting information, p. 2816 - 2819 (2015/03/18)
We report the preparation and new insight into photophysical properties of luminescent hydroxypyridonate complexes [MIIIL]- (M = Eu or Sm) of the versatile 3,4,3-LI(1,2-HOPO) ligand (L). We report the crystal structure of this ligand