Influence of trans-1,2-diaminocyclohexane structure and mixed carboxylic/phosphonic group combinations on samarium-153 chelation capacity and stability.
A simple procedure was developed to compare chelating agents for (153)Sm complexes as a preliminary step to synthesise bifunctional analogues. Several variables affecting the efficiency of complex stability were investigated, such as the pre-organisation concept, cavity size, and the nature of coordination sites. Four semi-rigid agents incorporating carboxylic and/or phosphonic groupings fixed at trans-1,2-diaminocyclohexane were evaluated for their (153)Sm chelation properties, and competition studies were performed. Data on the stability of the best chelating agent compound 3: trans-cyclohexane-1,2-bis(aminomethylphosphonic)-N,N'-bis(ethyl-2-iminodiacetic acid) in human serum are presented.
Ouadi
Ali
A
Chimie des bioconjugués, institut de biologie, U.463 Inserm, 9, quai Moncousu, 44093 Nantes cedex, France. ali.ouadi@ires.in2p3.fr
Loussouarn
Anthony
A
Morandeau
Laurence
L
Remaud
Patricia
P
Faivre-Chauvet
Alain
A
Webb
John
J
Gestin
Jean-Francois
JF
D002264:Carboxylic Acids / Q000737:chemistry*; D002614:Chelating Agents / Q000737:chemistry*; D003514:Cyclohexylamines / Q000138:chemical synthesis / Q000737:chemistry*; D004355:Drug Stability; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D008024:Ligands; D009942:Organometallic Compounds / Q000097:blood / Q000138:chemical synthesis / Q000737:chemistry*; D063065:Organophosphonates / Q000737:chemistry*; D009943:Organophosphorus Compounds / Q000737:chemistry; D011868:Radioisotopes; D012493:Samarium / Q000097:blood / Q000737:chemistry*
D002264:Carboxylic Acids; D002614:Chelating Agents; D003514:Cyclohexylamines; D008024:Ligands; D009942:Organometallic Compounds; D063065:Organophosphonates; D009943:Organophosphorus Compounds; D011868:Radioisotopes; D012493:Samarium; C030435:1,2-cyclohexanediamine