Synthesis of a poly(Gd(III)-DOTA)-PNA conjugate as a potential MRI contrast agent via post-synthetic click chemistry functionalization

Wang Xiaoxiao; Milne Mark; Martinez Francisco; Scholl Timothy J.; Hudson Robert H. E.

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Synthesis of a poly(Gd(III)-DOTA)-PNA conjugate as a potential MRI contrast agent via post-synthetic click chemistry functionalization

机译：通过合成后咔哒化学功能化合成聚（GD（III）-DOTA）-PNA缀合物作为潜在的MRI造影剂

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Herein we present a method for the simultaneous, multiple conjugation of alkynyl-(Gd(III)-DOTA) moieties to a PNA oligomer possessing a domain of azide residues. This is achieved in a single Huisgen type coppercatalyzed azide alkyne cycloaddition (CuAAC) reaction after the oligomer assembly is completed. A triplex formed between the labelled PNA and riboadenylic acid, [(Gd(III)-DOTA)(4)-PNA](2):poly(rA), displayed higher relaxivities at any field strength compared to the single-stranded probe at the same concentration of Gd3+ ions as determined by nuclear magnetic resonance dispersion (NMRD) studies.

机译：在此我们提出了一种用于同时，将炔基 - （GD（III）-DOTA）部分的多次缀合到具有叠氮残基结构域的PNA低聚物的方法。在低聚物组件完成后，这在单个Huisgen型铜催化叠氮化物丙烷炔环加入（Cuaac）反应中实现。在标记的PNA和核糖酰基酸之间形成的三重链式[（GD（III）-DOTA）（4）-PNA]（2）：聚（Ra），与单链探针相比，在任何场强处显示出更高的松弛性由核磁共振分散（NMRD）研究确定的相同浓度的GD3 +离子。

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《RSC Advances》 |2017年第71期|共5页
作者
Wang Xiaoxiao; Milne Mark; Martinez Francisco; Scholl Timothy J.; Hudson Robert H. E.;
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Univ Western Ontario Dept Chem 1151 Richmond St London ON N6A 5B7 Canada;

Univ Western Ontario Dept Chem 1151 Richmond St London ON N6A 5B7 Canada;

Univ Western Ontario Robarts Res Inst Dept Med Biophys 1151 Richmond St London ON N6A 5B7 Canada;

Univ Western Ontario Robarts Res Inst Dept Med Biophys 1151 Richmond St London ON N6A 5B7 Canada;

Univ Western Ontario Dept Chem 1151 Richmond St London ON N6A 5B7 Canada;

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正文语种 eng
中图分类化学;
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1. Synthesis of a poly(Gd(III)-DOTA)-PNA conjugate as a potential MRI contrast agent via post-synthetic click chemistry functionalization [J] . Wang Xiaoxiao, Milne Mark, Martinez Francisco, RSC Advances . 2017,第71期

机译：通过合成后咔哒化学功能化合成聚（GD（III）-DOTA）-PNA缀合物作为潜在的MRI造影剂
2. Design and synthesis of novel DOTA(Gd~(3+))-polymer conjugates as potential MRI contrast agents [J] . Mathurin Grogna, Rudi Cloots, Andre Luxen Journal of Materials Chemistry: An Interdisciplinary Journal dealing with Synthesis, Structures, Properties and Applications of Materials, Particulary Those Associated with Advanced Technology . 2011,第34期

机译：新型DOTA（Gd〜（3 +））-聚合物共轭物作为潜在MRI造影剂的设计与合成
3. Poly(para-phenylene ethynylene)s functionalized with Gd(III) chelates as potential MRI contrast agents [J] . Katelyn M. Atkins, Francisco M. Martinez, Ali Nazemi Canadian Journal of Chemistry . 2011,第1期

机译：Gd（III）螯合物官能化的聚对亚苯基乙炔基作为潜在的MRI造影剂
4. Functionalization of Amide-Building Blocks with endo-Gd-N-Cluster-Fullerene for Synthesis of BioShuttle Conjugates as cell-specific intracellular MR-Contrast Agents [C] . Pipkorn R, Wiessler M, Dunsch L, European Conference on Chemistry for Life Sciences . 2011

机译：酰胺基层与富烯族胺的官能化，用于合成BioShuttle缀合物作为细胞特异性细胞内MR-造影剂
5. Jacketed and functionalized poly(paraphenyleneethynylene)s: Nonaggregating conjugated polymers and materials functionalized through click-chemistry. [D] . Englert, Brian Carl. 2005

机译：带夹套和功能化的聚对苯乙炔：通过点击化学功能化的非聚集共轭聚合物和材料。
6. Lumazine Synthase Protein Nanoparticle-Gd(III)-DOTA Conjugate as a T1 contrast agent for high-field MRI [O] . YoungKyu Song, Young Ji Kang, Hoesu Jung, -1

机译：Lumazine合酶蛋白质纳米颗粒-Gd（III）-DOTA偶联物作为高场MRI的T1造影剂
7. Lumazine Synthase Protein Nanoparticle-Gd(III)-DOTA Conjugate as a T1 contrast agent for high-field MRI [O] . Song YoungKyu, Kang Young Ji, Jung Hoesu, 2015

机译：Lumazine合酶蛋白质纳米颗粒-Gd（III）-DOTA偶联物作为高场MRI的T1造影剂

Synthesis of a poly(Gd(III)-DOTA)-PNA conjugate as a potential MRI contrast agent via post-synthetic click chemistry functionalization

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