The Synthesis of D‐Trihydroxyllysine‐Based Oligopeptides as a Hydrophilic Scaffold and its Application to the Synthesis of Bifunctional Chelating Agents for Use as Bone Tracers |
| |
| Authors: | Hiroshi Tanaka Prof. Dr. Yoshio Ando Dr. Tsutomu Abe Dr. Takashi Takahashi Prof. Dr. |
| |
| Affiliation: | 1. Department of Applied Chemistry, Graduate School of Science and Engineering, Tokyo Institute of Technology, 2‐12‐1 Ookayama, Meguro, Tokyo 152‐8552 (Japan), Fax: (+81)?3‐5734‐2471;2. Nihon Medi‐Physics, 1, Kitasode, Sodegaura‐Shi, Chiba 299‐0266 (Japan) |
| |
| Abstract: | An effective hydrophilic scaffold composed of D ‐trihydroxyllysine‐based oligopeptides and its application in the synthesis of the various 111In–DTPA conjugates with mono‐ to penta‐bisphosphonate units for use as bone tracers are described. The D ‐trihydroxyllysine derivative with three orthogonal protecting groups was conjugated with functional devices at the γ position and allowed oligomerization based on peptide chemistry. The radiopharmaceutical complexes of 111InIII with selected chelators, 4 and 8 , were suitable for bone imaging. These results show that D ‐trihydroxyllysine 2 was an effective building block for the synthesis of multivalent ligands applicable to medical use. |
| |
| Keywords: | bisphosphonate chemical biology indium molecular imaging oligopeptides |
|
|
