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Synthesis, 99m Tc‐labeling, and preliminary biological evaluation of DTPA ‐melphalan conjugates
Author(s) -
Wang Jianjun,
Yang Wenjiang,
Xue Jinquan,
Zhang Yanhua,
Liu Yu
Publication year - 2017
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3575
Subject(s) - chemistry , chelation , conjugate , in vivo , melphalan , technetium 99m , linker , radiochemistry , nuclear chemistry , nuclear medicine , scintigraphy , organic chemistry , transplantation , medicine , mathematical analysis , mathematics , microbiology and biotechnology , surgery , computer science , biology , operating system
Melphalan (MFL) is a typical nitrogen mustard for the treatment of many types of cancer. For the purpose to develop novel 99m Tc‐labeled tumor imaging agents with SPECT, MFL was directly labeled by 99m Tc using diethylene triamine pentacetate acid (DTPA) as bifunctional chelating agent. The novel ligands were successfully synthesized by conjugation of DTPA to MFL to get monosubstituted DTPA‐MFL and bis‐substituted DTPA‐2MFL. Radiolabeling was performed in high yield to get 99m Tc‐DTPA‐MFL and 99m Tc‐DTPA‐2MFL, respectively, which were hydrophilic and stable at room temperature. The high initial tumor uptake with retention, good tumor/muscle ratios, and satisfactory scintigraphic images suggested the potential of 99m Tc‐DTPA‐MFL and 99m Tc‐DTPA‐2MFL for tumor imaging. However, the slow normal tissue clearance would be a great obstacle. Further modification on the linker and/or 99m Tc‐chelate to improve the tumor targeting efficacy and in vivo kinetic profiles is currently in progress.