反式-1,2-二氨基环己烷结构以及混合羧基/膦酸基团组合对钐-153螯合能力和稳定性的影响。

Influence of trans-1,2-diaminocyclohexane structure and mixed carboxylic/phosphonic group combinations on samarium-153 chelation capacity and stability.

作者信息

Ouadi Ali, Loussouarn Anthony, Morandeau Laurence, Remaud Patricia, Faivre-Chauvet Alain, Webb John, Gestin Jean-Francois

机构信息

Chimie des bioconjugués, institut de biologie, U.463 Inserm, 9, quai Moncousu, 44093 Nantes cedex, France.

出版信息

Eur J Med Chem. 2004 May;39(5):467-72. doi: 10.1016/j.ejmech.2004.02.009.

DOI:10.1016/j.ejmech.2004.02.009

PMID:15110973

Abstract

A simple procedure was developed to compare chelating agents for (153)Sm complexes as a preliminary step to synthesise bifunctional analogues. Several variables affecting the efficiency of complex stability were investigated, such as the pre-organisation concept, cavity size, and the nature of coordination sites. Four semi-rigid agents incorporating carboxylic and/or phosphonic groupings fixed at trans-1,2-diaminocyclohexane were evaluated for their (153)Sm chelation properties, and competition studies were performed. Data on the stability of the best chelating agent compound 3: trans-cyclohexane-1,2-bis(aminomethylphosphonic)-N,N'-bis(ethyl-2-iminodiacetic acid) in human serum are presented.

摘要

开发了一种简单的程序来比较用于（153）Sm配合物的螯合剂，作为合成双功能类似物的初步步骤。研究了几个影响配合物稳定性效率的变量，如预组织概念、空腔大小和配位位点的性质。评估了四种在反式-1,2-二氨基环己烷上固定有羧基和/或膦酸基团的半刚性试剂的（153）Sm螯合性能，并进行了竞争研究。给出了最佳螯合剂化合物3：反式环己烷-1,2-双（氨甲基膦酸）-N，N'-双（乙基-2-亚氨基二乙酸）在人血清中的稳定性数据。