99(m)Tc/Re complexes bearing bisnitroimidazole or mononitroimidazole as potential bioreductive markers for tumor: Synthesis, physicochemical characterization and biological evaluation

doi:10.1016/j.ejmech.2012.09.042

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	99(m)Tc/Re complexes bearing bisnitroimidazole or mononitroimidazole as potential bioreductive markers for tumor: Synthesis, physicochemical characterization and biological evaluation
	Mei, Lei; Wang, Yue; Chu, Taiwei
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2012-12-01
卷号	58 页码:50-63
关键词	Bisnitroimidazole Technetium Rhenium Tumor Hypoxia Biodistribution
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2012.09.042
英文摘要	Four monoamine-monoamide dithiol (MAMA) ligands containing two or one nitroimidazole moieties were synthesized and labeled with Tc-99m (labeling yield > 95%). The proposed structures of Tc-99m-complexes are identified by comparison with analogous Re-MAMA complexes. Tc-99m-MAMA complexes show better physicochemical characters than (TcO)-Tc-99m-(PnAO-1-(2-nitroimidazole)). Reduction potentials of nitro groups of the rhenium complexes are within the range for bioreductive compounds. As expected, biodistribution studies demonstrate that the 2-nitroimidazole complex shows better tumor-to-tissue ratios than 4-nitroimidazole analog for mononitroimidazole complexes, but not for MAMA-bisnitroimidazoles due to higher lipophilicity. Both the bisnitroimidazole compounds show rapider excretion, lower background activity in liver and higher tumor-to-tissue ratios than the mono-nitroimidazoles. Better biodistribution characteristic makes both the MAMA-bisnitroimidazole complexes, especially (TC)-T-99m-15, be potential tumor hypoxia marker. (C) 2012 Elsevier Masson SAS. All rights reserved.
语种	英语
出版者	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号	WOS:000312745100006
内容类型	期刊论文
源URL	[http://ir.iccas.ac.cn/handle/121111/49619]
专题	中国科学院化学研究所
通讯作者	Chu, Taiwei
作者单位	Peking Univ, Beijing Natl Lab Mol Sci, Radiochem & Radiat Chem Key Lab Fundamental Sci, Coll Chem & Mol Engn, Beijing 100871, Peoples R China
推荐引用方式 GB/T 7714	Mei, Lei,Wang, Yue,Chu, Taiwei. 99(m)Tc/Re complexes bearing bisnitroimidazole or mononitroimidazole as potential bioreductive markers for tumor: Synthesis, physicochemical characterization and biological evaluation[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,58:50-63.
APA	Mei, Lei,Wang, Yue,&Chu, Taiwei.(2012).99(m)Tc/Re complexes bearing bisnitroimidazole or mononitroimidazole as potential bioreductive markers for tumor: Synthesis, physicochemical characterization and biological evaluation.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,58,50-63.
MLA	Mei, Lei,et al."99(m)Tc/Re complexes bearing bisnitroimidazole or mononitroimidazole as potential bioreductive markers for tumor: Synthesis, physicochemical characterization and biological evaluation".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 58(2012):50-63.