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新型三齿-3,4-HOPO 镧系元素配合物作为潜在的成像探针:配合物稳定性和磁性。

New tris-3,4-HOPO lanthanide complexes as potential imaging probes: complex stability and magnetic properties.

机构信息

Centro de Química Estrutural, Instituto Superior Técnico, Universidade Técnica de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisboa, Portugal.

出版信息

Dalton Trans. 2013 May 7;42(17):6046-57. doi: 10.1039/c2dt32237d. Epub 2013 Jan 7.

Abstract

There is a growing interest in the development of new medical diagnostic tools with higher sensibility and less damage for the patient body, namely on imaging reporters for the management of diseases and optimization of treatment strategies. This article examines the properties of a new class of lanthanide complexes with a tripodal tris-3-hydroxy-4-pyridinone (tris-3,4-HOPO) ligand - NTP(PrHP)(3). Among the studies herein performed, major relevance is given to the thermodynamic stability of the complexes with a series of Ln(3+) ions (Ln = La, Pr, Gd, Er, Lu) and to the magnetic relaxation properties of the Gd(3+) complex. This hexadentate ligand enables the formation of (1 : 1) Ln(3+) complexes with high thermodynamic stability following the usual trend, while the Gd-chelates show improved relaxivity (higher hydration number), as compared with the commercially available Gd-based contrast agents (CAs); transmetallation of the Gd(3+)-L complex with Zn(2+) proved to be thermodynamically and kinetically disfavored. Therefore, NTP(PrHP)(3) emerges as part of a recently proposed new generation of CAs with prospective imaging sensibility gains.

摘要

人们越来越关注开发具有更高灵敏度和对患者身体损伤更小的新型医学诊断工具,即用于疾病管理和治疗策略优化的成像报告剂。本文研究了一类新型镧系金属配合物的性质,该配合物具有三脚架三-3-羟基-4-吡啶酮(三-3,4-HOPO)配体 - NTP(PrHP)(3)。在本文进行的研究中,主要关注一系列 Ln(3+)离子(Ln = La、Pr、Gd、Er、Lu)与配合物的热力学稳定性,以及 Gd(3+)配合物的磁弛豫性质。这种六配位配体能够形成具有高热力学稳定性的(1 : 1)Ln(3+)配合物,遵循通常的趋势,而与市售的基于 Gd 的造影剂(CA)相比,Gd-配合物显示出更好的弛豫率(更高的水合数);用 Zn(2+)进行 Gd(3+)-L 配合物的转金属化被证明在热力学和动力学上都是不利的。因此,NTP(PrHP)(3)成为最近提出的新一代 CAs 的一部分,具有潜在的成像灵敏度增益。

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