Thymidine derivates as well as preparation method and applications thereof in preparing tumor developing agents as ligand

Abstract

The invention discloses thymidine derivates, belonging to the technical field of radiopharmaceutical chemistry and clinical nuclear medicine. A molecular formula of the derivates is N<3>-{N'-[(2-mercaptoethylamine)acetyl]-2-aminoethylsulphydryl-1-hexoamide}-thymidine (short for NHT). The invention further provides a preparation method for the thymidine derivates, as well as applications of the thymidine derivates in preparing tumor developing agents as ligand with <99m>Tc to form complex. Marker <99m>Tc in <99m>Tc-NHT has high radiochemical purity; lipd / water partition coefficient logP is 0.76; the stability is good; the safety of animal experiment is higher; and the ratios of radioactivity absorbed by tumor with radioactivity absorbed by muscle, radioactivity absorbed by bone and radioactivity absorbed by blood according to ID / g by percent are respectively 4.41, 2.45 and 1.51, therefore, the thymidine derivates can be used as a novel tumor developer for tumor diagnosis.

Description

technical field [0001] The invention relates to the technical fields of radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a thymidine derivative, its preparation method and its use as a ligand in the preparation of a tumor imaging agent. Background technique [0002] Tumor is one of the diseases that seriously threaten human life. Radionuclide imaging can reflect changes in the physiology, pathology, metabolism and function of tumors, and radionuclide imaging is a non-invasive detection method. Many advantages make radionuclide Imaging has become the main method of tumor diagnosis. [0003] Among them, radionuclide-labeled nucleosides are a class of molecular probes that develop rapidly, such as 18 F-labeled thymidines 18 F-FLT, 18 F-FLT indirectly reflects cell proliferation by reflecting DNA synthesis. Clinical studies have shown that 18 F-FLT has unique application prospects in the detection of tumor cell proliferation, such as chest tumor...

AI Technical Summary

Problems solved by technology

However 18 F-FLT is a positron tracer that requires an accelerator to generate fluorine (18), which is expensive; in contrast, 99m Tc has significant advantages such as short half-life (6.02 hours), suitable gamma-ray energy (140 keV), convenient acquisition from molybdenum-technetium generators, and low price. It is the most common radionuclide used in SPECT imaging. Therefore, the development Successful SPECT tracers can significantly reduce examination costs and reduce the burden on patients, which has important economic and social significance

Images