Reagents for astatination of biomolecules. 3. Comparison of closo-decaborate(2-) and closo-dodecaborate(2-) moieties as reactive groups for labeling with astatine-211.

ABSTRACT: In vivo deastatination has been a major problem in the development of reagents for therapeutic applications of the alpha-particle emitting radionuclide (211)At. Our prior studies demonstrated that the use of a closo-decaborate(2-) ([closo-B(10)H(9)R](2-)) moiety for (211)At labeling of biomolecules provides conjugates that are stable to in vivo deastatination. In this investigation, the closo-decaborate(2-) moiety was compared with the structurally similar closo-dodecaborate(2-) ([closo-B(12)H(11)R](2-)) to determine if one has more favorable properties than the other for use in pendant groups as (211)At labeling molecules. To determine the differences, two sets of structurally identical molecules, with the exception that they contained either a closo-decaborate(2-) or a closo-dodecaborate

SUBMITTER: Wilbur DS 

PROVIDER: S-EPMC2668518 | biostudies-literature | 2009 Mar

REPOSITORIES: biostudies-literature