Synthesis and Stability Evaluation of New HYNIC Derivatives as Ligands for Technetium-99m

被引：3

作者：

Joyard, Yoann ^{[1
,2
,3
,4
]}

Bischoff, Laurent ^{[4
]}

Levacher, Vincent ^{[4
]}

Papamicel, Cyril ^{[4
]}

Vera, Pierre ^{[1
,2
,3
]}

Bohn, Pierre ^{[1
,2
,3
]}

机构：

[1] Ctr Henri Becquerel, Dept Nucl Med, F-76038 Rouen, France

[2] Rouen Univ Hosp, F-76038 Rouen, France

[3] QuantIF LITIS, EA4108, F-76038 Rouen, France

[4] IRCOF Rouen, F-76130 Mont St Aignan, France

来源：

LETTERS IN ORGANIC CHEMISTRY | 2014年 / 11卷 / 03期

关键词：

Technetium-99m; HYNIC; 2-nitroimidazole; tumor hypoxia; imaging; stability evaluation; HYPOXIA IMAGING AGENT; IN-VIVO EVALUATION; TUMOR HYPOXIA; IODOAZOMYCIN ARABINOSIDE; FOCAL SITES; COMPLEX; BIODISTRIBUTION; INFECTION; ANALOGS; MARKER;

D O I：

10.2174/15701786113106660087

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An efficient synthetic route to prepare two new HYNIC derivatives with a 2-nitroimidazole moiety designed for tumor hypoxia imaging is described. During the course of the synthesis, the optimization of N-alkylation reaction of 2-nitroimidazole with propargyl bromide is reported to favor the formation of the terminal alkyne versus allene. Thereafter, the two ligands were used with tricine/EDDA to complex Tc-99m. However, decomposition of these ligands was observed and we suggest a reasonable explanation based on LC-MS analysis.

引用

页码：208 / 214

页数：7

共 50 条

[31] Synthesis and biological evaluation of a technetium-99m(I)-tricarbonyl-labelled phenyltropane derivative [J].

Kieffer, DM ;

Cleynhens, BJ ;

Vanbilloen, HP ;

Rattat, D ;

Terwinghe, CY ;

Mortelmans, L ;

Bormans, GM ;

Verbruggen, AA .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (02) :382-386

[32] Organic synthesis and biological evaluation of novel "3+1" mixed ligands of technetium-99m Gabapentin as receptor imaging agents [J].

Amin, A. M. ;

Abou Zid, K. ;

Bayoumi, N. A. ;

Abd El-hamid, M. .

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, 2010, 283 (01) :55-62

[33] Evaluation of a technetium-99m labeled bombesin homodimer for GRPR imaging in prostate cancer [J].

Zilin Yu ;

Giuseppe Carlucci ;

Hildo J. K. Ananias ;

Rudi A. J. O. Dierckx ;

Shuang Liu ;

Wijnand Helfrich ;

Fan Wang ;

Igle J. de Jong ;

Philip H. Elsinga .

Amino Acids, 2013, 44 :543-553

[34] Technetium-99m labeling and evaluation of olsalazine: a novel agent for ulcerative colitis imaging [J].

El-Kawy, O. A. ;

Ibrahim, I. T. ;

Farah, K. .

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2015, 58 (08) :336-341

[35] Evaluation of the cytotoxic and mutagenic potentiality of technetium-99m in Escherichia coli [J].

Silva, CR ;

Valsa, JO ;

Caldeira-de-Araújo, A ;

Amaral, A ;

Bernardo, M .

CELLULAR AND MOLECULAR BIOLOGY, 2002, 48 (07) :783-787

[36] Technetium-99m radiochemistry for pharmaceutical applications [J].

Papagiannopoulou, Dionysia .

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2017, 60 (11) :502-520

[37] RADIOLABELLING OF GLYCOSYLATED SOMATOSTATIN WITH TECHNETIUM-99m [J].

He, C. ;

Zhai, S. ;

Cui, H. ;

Du, J. .

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2005, 48 :S237-S237

[38] Synthesis of S-thiomethyl DMSA and S-thiomethyl ECD, radiolabelling with technetium-99m and biological evaluation [J].

Sanyal, Kasturi ;

Debnath, Mita Chatterjee .

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2012, 55 (07) :258-263

[39] Synthesis and biological evaluation of technetium-99m labeled galactose derivatives as potential asialoglycoprotein receptor probes in a hepatic fibrosis mouse model [J].

Chang, Wen-Yi ;

Kao, Hao-Wen ;

Wang, Hsin-Ell ;

Chen, Jenn-Tzong ;

Lin, Wuu-Jyh ;

Wang, Shyh-Jen ;

Chen, Chuan-Lin .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (23) :6486-6491

[40] Synthesis of S-thiomethyl MAG3, radiolabelling with technetium-99m and biological evaluation [J].

Sanyal, Kasturi ;

Chattopadhyay, Sankha ;

Debnath, Mita Chatterjee .

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2012, 55 (10) :377-382

← 1 2 3 4 5 →