- Thermodynamic Stability and Speciation of Ga(III) and Zr(IV) Complexes with High-Denticity Hydroxamate Chelators
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Increasing attention has been recently devoted to 89Zr(IV) and 68Ga(III) radionuclides, due to their favorable decay characteristics for positron emission tomography (PET). In the present paper, a deep investigation is presented on Ga(III) and Zr(IV) comp
- Albanese, Valentina,Baldi, Andrea,Fritsky, Igor O.,Guerrini, Remo,Gumienna-Kontecka, Elzbieta,Illuminati, Davide,Mular, Andrzej,Ostrowska, Ma?gorzata,Pacifico, Salvatore,Piasta, Karolina,Remelli, Maurizio,Toporivska, Yuliya
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- Rational Design, Development, and Stability Assessment of a Macrocyclic Four-Hydroxamate-Bearing Bifunctional Chelating Agent for 89Zr
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Zirconium-89 is a positron-emitting radionuclide of high interest for medical imaging applications with positron emission tomography (PET). For the introduction of this radiometal into biologically active targeting vectors, the chelating agent desferrioxa
- Seibold, Uwe,W?ngler, Bj?rn,W?ngler, Carmen
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p. 1555 - 1571
(2017/09/26)
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- Octadentate Zirconium(IV)-Loaded Macrocycles with Varied Stoichiometry Assembled From Hydroxamic Acid Monomers using Metal-Templated Synthesis
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The reaction between Zr(IV) and the forward endo-hydroxamic acid monomer 4-[(5-aminopentyl)(hydroxy)amino]-4-oxobutanoic acid (for-PBH) in a 1:4 stoichiometry in the presence of diphenylphosphoryl azide and triethylamine gave the octadentate Zr(IV)-loaded tetrameric hydroxamic acid macrocycle for-[Zr(DFOT1)] ([M + H]+ calc 887.3, obs 887.2). In this metal-templated synthesis (MTS) approach, the coordination preferences of Zr(IV) directed the preorganization of four oxygen-rich bidentate for-PBH ligands about the metal ion prior to ring closure under peptide coupling conditions. The replacement of for-PBH with 5-[(5-aminopentyl) (hydroxy)amino]-5-oxopentanoic acid (for-PPH), which contained an additional methylene group in the dicarboxylic acid region of the monomer, gave the analogous Zr(IV)-loaded macrocycle for-[Zr(PPDFOT1)] ([M + H]+ calc 943.4, obs 943.1). A second, well-resolved peak in the liquid chromatogram from the for-PPH MTS system also characterized as a species with [M + H]+ 943.3, and was identified as the octadentate complex between Zr(IV) and two dimeric tetradentate hydroxamic acid macrocycles for-[Zr(PPDFOT1D)2]. Treatment of for-[Zr(PPDFOT1)] or for-[Zr(PPDFOT1D)2] with EDTA at pH 4.0 gave the respective hydroxamic acid macrocycles as free ligands: octadentate PPDFOT1 or two equivalents of tetradentate PPDFOT1D (homobisucaberin, HBC). At pH values closer to physiological, EDTA treatment of for-[Zr(DFOT1)], for-[Zr(PPDFOT1)], or Zr(IV) complexes with related linear tri- or tetrameric hydroxamic acid ligands showed the macrocycles were more resistant to the release of Zr(IV), which has implications for the design of ligands optimized for the use of Zr(IV)-89 in positron emission tomography (PET) imaging of cancer.
- Tieu, William,Lifa, Tulip,Katsifis, Andrew,Codd, Rachel
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supporting information
p. 3719 - 3728
(2017/03/24)
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- Evaluation of hadacidin analogues
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Several derivatives of hadacidin have been developed and evaluated for activity against adenylosuccinate synthetase.
- Tibrewal, Nidhi,Elliott, Gregory I.
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supporting information; experimental part
p. 517 - 519
(2011/02/25)
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- ALKYLATION OF N-BENZYLOXYUREAS AND CARBAMATES
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N-benzyloxyureas and orthogonically protected N-hydroxycarbamates can be alkylated in high yields and subsequently deprotected to provide N-alkyl hydroxyureas and hydroxylamines.
- Sulsky, Richard,Demers, James P.
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