Conjugates of Gd(III) Complexes to Di- and Tri-hydroxy Substituted Cholanoic Acids: Regioselective Oxidation with Hydroxysteroid Dehydrogenases

The preparative-scale oxidation of Gd(III) complexes of ligands containing 7,12-dihydroxy and 12-hydroxy substituted cholanoic moieties to the corresponding 12-oxo derivatives was accomplished by means of 12 &#102 -hydroxysteroid dehydrogenase. The enzymatic transformation appeared preferable to the chemical one because it was highly regioselective and environmentally benign. Other dehydrogenases, namely 3 &#102 - and 7 &#102 -hydroxysteroid dehydrogenases, also proved to be capable of catalysing the regioselective oxidation of the hydroxy groups of a Gd(III) complex containing a subunit of 3,7,12-trihydroxycholanoic acid. The above complexes are of interest as contrast agents for in vivo magnetic resonance imaging.