Vinyl substituted radiohalogen conjugates for protein labeling.

摘要

Vinyl radiohalogenated small molecules as shown in formulae I and II: wherein *X is a radiohalogen, C=C is a double bond, R1 and R2 represent a hydrogen atom; alkyl or substituted alkyl group, an aryl or substituted aryl group, a heteroalkyl group, a heteroaryl group, or a mixed alkylaryl group. Y represents any of the groups as for R1 and R2, except that Y cannot be hydrogen, and bearing a functional group suitable for binding to protein under conditions that preserve the biological activity of the protein. The compounds of formulae I and II can be coupled to proteins such as monoclonal antibodies to provide reagents for diagnostic and therapeutic applications. Also metalated precursors of compounds I and II, as well as radiopharmaceutical reagent kits containing any of the subject small molecules.