Preparation And Primary Biological Evaluation Of ～(188)ReN Complexes

TDD and its derivatives are excellent ligands, and their ¹⁸⁸Re labeledcompounds are highly lipophilic. The solutions of lipiodol of these ¹⁸⁸Re labeledcompounds could accumulate in liver tumour by performing transcatheter arterialembolization, so that they might be potential radiopharmaceuticals for liver cancer.But the radiolabeling yields of these compounds are poor and it is necessary toimprove the retention of their lipiodol solutions in liver tumour.Base on the structure of TDD, we designed and synthesized three N-piperidinylethyl-TDD derivatives that was NEPTDD, NEMPTDD andNEMMPTDD. We improved the methods in ¹⁸⁸Re labeling process by comparingthe effects of different donors of nitrido nitrogen atoms and adding oxalate asactivator, then we got three ¹⁸⁸ReN compounds with high yield that beyond 95%.These compounds were stable in vitro and could dissolve in lipiodol easily. Theanimal experiments in normal mice showed that the three ¹⁸⁸ReN compoundseliminated quickly from mice and there were some uptake in liver. We hadestablished rabbits liver cancer models with VX-2 carcinoma and performed TAEto evaluate biological properties of the lipiodol solutions of the three ¹⁸⁸ReNcompounds. The results of SPECT showed that there were high uptake and longtime retention in liver tumours. It indicated that these lipiodol solutions of the¹⁸⁸ReN compounds could be promising radiopharmaceuticals for liver cancer.