Monooxorhenium(V) complexes with 222-N₂S₂ MAMA ligands for bifunctional chelator agents: Syntheses and preliminary in vivo evaluation.

ABSTRACT:

Introduction

Targeted radiotherapy using the bifunctional chelate approach with ^186/188Re(V) is challenging because of the susceptibility of monooxorhenium(V)-based complexes to oxidize in vivo at high dilution. A monoamine-monoamide dithiol (MAMA)-based bifunctional chelating agent was evaluated with both rhenium and technetium to determine its utility for in vivo applications.

Methods

A 222-MAMA chelator, 222-MAMA(N-6-Ahx-OEt) bifunctional chelator, and 222-MAMA(N-6-Ahx-BBN(7-14)NH₂) were synthesized, complexed with rhenium, radiolabeled with ^99mTc and ¹⁸⁶Re (carrier added and no carrier added), and evaluated in initial biological distribution studies.

Results

An IC₅₀ value of 2.0±0.7nM for ^natReO-222

SUBMITTER: Demoin DW 

PROVIDER: S-EPMC5118109 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature