Triaza-based amphiphilic chelators: synthetic route, in vitro characterization and in vivo studies of their Ga(III) and Al(III) chelates

Journal of Inorganic Biochemistry
Arsénio de SáJoão P André

Abstract

Radiogallium chelates are important for diagnostic imaging in nuclear medicine (PET (positron emission tomography) and gamma-scintigraphy). Micelles are adequate colloidal vehicles for the delivery of therapeutic and diagnostic agents to organs and tissues. In this paper we describe the synthesis and in vitro and in vivo studies of a series of micelles-forming Ga(III) chelates targeted for the liver. The amphiphilic ligands are based on NOTA (NOTA=1,4,7-triazacyclonoane-N,N'N''-triacetic acid) and bear a alpha-alkyl chain in one of the pendant acetate arms (the size of the chain changes from four to fourteen carbon atoms). A multinuclear NMR study ((1)H, (13)C, (27)Al and (71)Ga) gave some insights into the structure and dynamics of the metal chelates in solution, consistent with their rigidity and octahedral or pseudo-octahedral geometry. The critical micellar concentration of the chelates was determined using a fluorescence method and (27)Al NMR spectroscopy (Al(III) was used as a surrogate of Ga(III)), both showing similar results and suggesting that the chelates of NOTAC6 form pre-micellar aggregates. The logP (octanol-water) determination showed enhancement of the lipophilic character of the Ga(III) chelates with the incre...Continue Reading

Citations

Apr 11, 2014·Dalton Transactions : an International Journal of Inorganic Chemistry·Miguel F FerreiraCarlos F G C Geraldes
Aug 3, 2011·Bioconjugate Chemistry·Christopher A D'SouzaDavid M Goldenberg
May 22, 2013·European Journal of Medicinal Chemistry·Pooja SrivastavaAnil K Mishra
Apr 16, 2011·Nuclear Medicine and Biology·André FontesJoão P André
Apr 23, 2013·Contrast Media & Molecular Imaging·Ingrid DijkgraafOtto C Boerman
Feb 19, 2014·Nuclear Medicine and Biology·Malgorzata LipowskaAndrew T Taylor
Apr 5, 2016·Dalton Transactions : an International Journal of Inorganic Chemistry·Mariane Le FurRaphaël Tripier
Nov 10, 2015·Chemical Society Reviews·Kantapat ChansaenpakFrançois P Gabbaï
Oct 14, 2020·Wiley Interdisciplinary Reviews. Nanomedicine and Nanobiotechnology·Shahab Ranjbar BahadoriXiankai Sun

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