Choudhry, U. and Greenland, W.E.P. and Goddard, W.A. and Maclennan, T.A.J. and Teat, S.J. and Blower, P.J. (2003) New routes to bioconjugates of rhenium using the oxobis(dithiolato)rhenate(v) core. DALTON TRANSACTIONS (3). pp. 311-317. ISSN 1477-9226.
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The development of the rhenium-188 generator has provided a convenient and economic source of radionuclide for targeted radionuclide therapy of cancer. To exploit this more widely, mild, convenient and efficient methods for stable incorporation of the radionuclide into biomolecules are required. The aim of this work is to exploit the tumour targeting therapeutic radiopharmaceutical [ReO(dmsa)(2)](-) (H(2)dmsa = meso-dimercaptosuccinic acid), which is easily synthesised in radioactive form and highly stable in vivo, for this purpose. A new efficient synthesis of [ReO(dmsa)(2)](-), as a single isomer (syn-endo), from perrhenate using acetylhydrazine as reductant, is reported. Dehydration of the two dicarboxylic acid groups of [ReO(dmsa)(2)](-) with dicyclohexylcarbodiimide gives the yellow cyclic dianhydride [ReO(dmsaa)(2)](-) (H(2)dmsaa = meso-dimercaptosuccinic anhydride) without disrupting the ReOS4 core. As its tetraethylammonium salt, [ReO(dmsaa)(2)](-) was characterised crystallographically as a distorted square pyramidal complex with an axial oxo-group and a syn-endo orientation of the two anhydride rings with respect to this oxo-group. [ReO(dmsaa)(2)](-) reacts with primary and secondary amines including lysine residues of peptides, to form amide-linked conjugates, which were identified by ES-MS. The syntheses are fast, efficient and employ mild conditions, making them readily adaptable for a kit-based approach to rhenium and technetium radiopharmaceuticals.
|Additional information:||Article 651VB English Times Cited:1 Cited References Count:47|
|Uncontrolled keywords:||RE-188 DIMERCAPTOSUCCINIC ACID IN-VITRO STABILITY MONOCLONAL-ANTIBODIES TARGETED RADIOTHERAPY THIOETHER COMPLEXES CRYSTAL-STRUCTURES QUALITY-CONTROL BLADDER-CANCER TC-99M RADIOIMMUNOTHERAPY|
|Divisions:||Faculties > Science Technology and Medical Studies > School of Biosciences|
|Depositing User:||Sue Davies|
|Date Deposited:||09 Sep 2008 09:42|
|Last Modified:||11 Jun 2012 13:58|
|Resource URI:||http://kar.kent.ac.uk/id/eprint/7164 (The current URI for this page, for reference purposes)|
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