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新型N2S2供体大环配体铜(II)配合物的合成与表征:(64)Cu配合物的合成及体内评价

Synthesis and characterization of the copper(II) complexes of new N2S2-donor macrocyclic ligands: synthesis and in vivo evaluation of the (64)Cu complexes.

作者信息

Papini Grazia, Alidori Simone, Lewis Jason S, Reichert David E, Pellei Maura, Gioia Lobbia Giancarlo, Biddlecombe Gráinne B, Anderson Carolyn J, Santini Carlo

机构信息

Dipartimento di Scienze Chimiche, Università di Camerino, via S. Agostino 1, 62032, Camerino, MC, Italy.

出版信息

Dalton Trans. 2009 Jan 7(1):177-84. doi: 10.1039/b808831d. Epub 2008 Nov 4.

DOI:10.1039/b808831d
PMID:19081987
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4418490/
Abstract

The aim of this work was to prepare a novel class of (64)Cu(II) labeled complexes with the new macrocyclic ligands 1,10-dithia-4,7-diazacyclododecane-3,8-dicarboxylic acid (NEC-SE, 1), 1,10-dithia-4,7-diazacyclotridecane-3,8-dicarboxylic acid (NEC-SP, 2) and 1,10-dithia-4,7-diazacyclotetradecane-3,8-dicarboxylic acid, (NEC-SB, 3 ) to evaluate the usefulness of these macrocycles for potential utility as (64)Cu(II) chelators. The corresponding non-radioactive complexes [Cu(NEC-SE)] x 3H(2)O (4), [Cu(NEC-SP)] x 3H(2)O (5) and [Cu(NEC-SB)] (6) were prepared and their (64)Cu-analogs, [(64)Cu(NEC-SE)] (7) and [(64)Cu(NEC-SP)] (8) and [(64)Cu(NEC-SB)] (9) were produced in >98% radiochemical purity. Rats were injected with complex 7, 8 or 9 and were euthanized at 1, 4 and 24 h. All three complexes are cleared from the blood over the first hour following injection but there is poor clearance of this activity over 24 h. A similar pattern of retention was noted in the liver where the levels of activity in this tissue at 1 h are not statistically different from those at 24 h. Molecular mechanics and DFT studies were performed on the complexes in order to gain insight into the lower stability.

摘要

这项工作的目的是制备一类新型的用新型大环配体1,10 - 二硫杂 - 4,7 - 二氮杂环十二烷 - 3,8 - 二羧酸(NEC - SE,1)、1,10 - 二硫杂 - 4,7 - 二氮杂环十三烷 - 3,8 - 二羧酸(NEC - SP,2)和1,10 - 二硫杂 - 4,7 - 二氮杂环十四烷 - 3,8 - 二羧酸(NEC - SB,3)标记的(64)Cu(II)配合物,以评估这些大环作为(64)Cu(II)螯合剂的潜在用途。制备了相应的非放射性配合物[Cu(NEC - SE)]·3H₂O(4)、[Cu(NEC - SP)]·3H₂O(5)和[Cu(NEC - SB)](6),并制备了它们的(64)Cu类似物[(64)Cu(NEC - SE)](7)、[(64)Cu(NEC - SP)](8)和[(64)Cu(NEC - SB)](9),其放射化学纯度>98%。给大鼠注射配合物7、8或9,并在1、4和24小时后实施安乐死。注射后的第一个小时内,所有三种配合物都从血液中清除,但在24小时内这种活性清除不佳。在肝脏中也观察到类似的滞留模式,该组织在1小时时的活性水平与24小时时的活性水平在统计学上没有差异。对这些配合物进行了分子力学和密度泛函理论研究,以便深入了解其较低的稳定性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/253a/4418490/4de50f9f2a61/nihms681709f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/253a/4418490/035d43f94757/nihms681709f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/253a/4418490/71cd2f141afc/nihms681709f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/253a/4418490/bd4a9b1b2998/nihms681709f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/253a/4418490/4de50f9f2a61/nihms681709f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/253a/4418490/035d43f94757/nihms681709f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/253a/4418490/71cd2f141afc/nihms681709f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/253a/4418490/bd4a9b1b2998/nihms681709f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/253a/4418490/4de50f9f2a61/nihms681709f4.jpg

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