116989-51-6Relevant articles and documents
Synthesis and evaluation of technetium-99m-labeled bioreductive pharmacophores conjugated with amino acids and peptides for tumor imaging
Baishya, Rinku,Nayak, Dipak K.,Karmakar, Sanmoy,Chattopadhyay, Sankha,Sachdeva, Satbir S.,Sarkar, Bharat R.,Ganguly, Shantanu,Debnath, Mita C.
, p. 504 - 517 (2015)
Development of molecular imaging agents to target tumor has become a major trend in nuclear medicine. With the aim to develop new potential 99mTc-radiopharmaceuticals for targeting tumor, we have synthesized 5-nitroimidazolyl amino acids and RGD-coupled 2-nitroimidazoles. Technetium-99m radiolabeling with high radiochemical purity (>90%) was achieved for all the compounds. The radiolabeled complexes exhibited substantial in vitro stability in saline, serum, and histidine solution (10-2 m). Cell binding studies in EAC and B16F10 cell lines also revealed rapid and comparatively high cellular internalization. Among all the compounds studied, the binding of 99mTc(CO)3-5 to B16F10 cells was moderately inhibited by the competitive peptide c[RGDfV], suggesting specificity of the radioligand toward αvβ3 receptor. However, no significant displacement of bound radioligand was observed when the binding of the 99mTc-labeled complexes to above cells was challenged with excess competitive peptide. Fluorescent microscopy study provided direct evidence of intracellular localization of 5(6)-carboxyfluorescein-labeled 2-nitroimidazolyl-RGD-peptide in αvβ3-positive B16F10 mouse melanoma cell line. The ligands caused only 8-13% of hemolysis toward rat erythrocytes at concentrations as high as 100 μm. Imaging and biodistribution studies were performed in Swiss albino mice bearing induced tumor. 99mTc-1 and 99mTc(CO)3-5 demonstrated a very favorable in vivo profile. Selective uptake and retention in tumor with encouraging tumor/muscle and tumor/blood ratio and significant cellular uptake of fluorescence-labeled-2-nitroimidazolyl RGD indicate the great potentiality of the pharmacophore for further evaluation as potential molecular imaging agent in cancer diagnosis.
Synthesis and stability evaluation of new HYNIC derivatives as ligands for Technetium-99m
Joyard, Yoann,Bischoff, Laurent,Levacher, Vincent,Papamicael, Cyril,Vera, Pierre,Bohn, Pierre
, p. 208 - 214 (2014/05/20)
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 99mTc. However, decomposition of these ligands was observed and we suggest a reasonable explanation based on LC-MS analysis.
Synthesis of 68Ga-labeled DOTA-nitroimidazole derivatives and their feasibilities as hypoxia imaging PET tracers
Hoigebazar, Lathika,Jeong, Jae Min,Hong, Mee Kyung,Kim, Young Ju,Lee, Ji Youn,Shetty, Dinesh,Lee, Yun-Sang,Lee, Dong Soo,Chung, June-Key,Lee, Myung Chul
experimental part, p. 2176 - 2181 (2011/05/07)
The imaging of hypoxia is important for therapeutic decision making in various diseases. 68Ga is an important radionuclide for positron emission tomography (PET), and its usage is increasing, due to the development of the 68Ge/6
