DOTA derivative - CAS 153777-70-9
Catalog number: 153777-70-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
DOTA derivative is a benxyl derivative of the cyclic tosamide; can be nitrated directly; is more convenient to incorporate the nitro group after deprotection lithium aluminum hydride.
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DOTA derivative
1.New synthesis of phenyl-isothiocyanate C-functionalised cyclams. Bioconjugation and (64)Cu phenotypic PET imaging studies of multiple myeloma with the te2a derivative.
Halime Z1, Frindel M2, Camus N1, Orain PY1, Lacombe M3, Chérel M3, Gestin JF3, Faivre-Chauvet A3, Tripier R1. Org Biomol Chem. 2015 Dec 14;13(46):11302-14. doi: 10.1039/c5ob01618e.
Azamacrocyclic bifunctional chelating agents (BCAs) are essential for the development of radiopharmaceuticals in nuclear medicine and we wish to prove that their bioconjugation by a function present on a carbon atom of the macrocyclic skeleton is a solution of choice to maintain their in vivo inertness. Based on our very recent methodology using a bisaminal template and selective N-alkylation approach, a new synthesis of conjugable C-functionalised teta, te2a and cb-te2a has been developed. These chelators have indeed a growing interest in nuclear medicine for positron emission tomography (PET) and radioimmunotherapy (RIT) where they show in several cases better complexation properties than dota or dota-like macrocycles, especially with (64)Cu or (67)Cu radioisotopes. Chelators are bearing an isothiocyanate grafting function introduced by C-alkylation to avoid as much as possible a critical decrease of their chelating properties. The synthesis is very efficient and yields the targeted ligands, teta-Ph-NCS, te2a-Ph-NCS and cb-te2a-Ph-NCS without fastidious work-up and could be easily extended to other cyclam based-BCAs.
2.Ln(iii)-complexes of a DOTA analogue with an ethylenediamine pendant arm as pH-responsive PARACEST contrast agents.
Krchová T1, Gálisová A2, Jirák D3, Hermann P1, Kotek J1. Dalton Trans. 2016 Feb 16;45(8):3486-96. doi: 10.1039/c5dt04443j.
A novel macrocyclic DO3A derivative containing a linear diamine pendant arm, H3do3aNN, was prepared and its protonation and complexation properties were studied by means of potentiometry. It determined ligand consecutive protonation constants log KAn = 12.62, 10.28, 9.67, 8.30, 3.30 and 1.58 and stability constants of selected lanthanide (Eu(iii), Yb(iii)) complexes log KEuL = 23.16 and log KYbL = 22.76. The complexes could be protonated on the pendant amino group(s) with log K(HLM) ≈ 5.6 and log K(H2LM) ≈ 4.8. Solution structures of both complexes were studied by NMR spectroscopy. The study revealed that the complex species exist exclusively in the form of twisted-square-antiprismatic (TSA) isomers. The complexes show significant pH dependence of the Chemical Exchange Saturation Transfer (CEST) between their amino groups and the bulk water molecules in the pH range of 5-8. Thus, the pH dependence of the magnetization transfer ratio of CEST signals can be used for pH determination using magnetic resonance imaging techniques in a pH range relevant for in vivo conditions.
3.Cellular Uptake and Photo-Cytotoxicity of a Gadolinium(III)-DOTA-Naphthalimide Complex "Clicked" to a Lipidated Tat Peptide.
O'Malley WI1, Rubbiani R2, Aulsebrook ML3, Grace MR4, Spiccia L5, Tuck KL6, Gasser G7, Graham B8. Molecules. 2016 Feb 5;21(2). pii: E194. doi: 10.3390/molecules21020194.
A new bifunctional macrocyclic chelator featuring a conjugatable alkynyl-naphthalimide fluorophore pendant group has been prepared and its Gd(III) complex coupled to a cell-penetrating lipidated azido-Tat peptide derivative using Cu(I)-catalysed "click" chemistry. The resulting fluorescent conjugate is able to enter CAL-33 tongue squamous carcinoma cells, as revealed by confocal microscopy, producing a very modest anti-proliferative effect (IC50 = 93 µM). Due to the photo-reactivity of the naphthalimide moiety, however, the conjugate's cytotoxicity is significantly enhanced (IC50 = 16 µM) upon brief low-power UV-A irradiation.
4.Associating a negatively charged GdDOTA-derivative to the Pittsburgh compound B for targeting Aβ amyloid aggregates.
Martins AF1,2,3,4, Oliveira AC3, Morfin JF1, Laurents DV5, Tóth É1, Geraldes CF6,7. J Biol Inorg Chem. 2016 Mar;21(1):83-99. doi: 10.1007/s00775-015-1316-9. Epub 2015 Nov 27.
We have conjugated the tetraazacyclododecane-tetraacetate (DOTA) chelator to Pittsburgh compound B (PiB) forming negatively charged lanthanide complexes, Ln(L4), with targeting capabilities towards aggregated amyloid peptides. The amphiphilic Gd(L4) chelate undergoes micellar aggregation in aqueous solution, with a critical micellar concentration of 0.68 mM, lower than those for the neutral complexes of similar structure. A variable temperature (17)O NMR and NMRD study allowed the assessment of the water exchange rate, k ex (298)  = 9.7 × 10(6) s(-1), about the double of GdDOTA, and for the description of the rotational dynamics for both the monomeric and the micellar forms of Gd(L4). With respect to the analogous neutral complexes, the negative charge induces a significant rigidity of the micelles formed, which is reflected by slower and more restricted local motion of the Gd(3+) centers as evidenced by higher relaxivities at 20-60 MHz.
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CAS 153777-70-9 DOTA derivative

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