Synthesis of new carbon-11-labeled 7-aroyl-aminoindoline-1-sulfonamides as potential PET agents for imaging of tubulin polymerization in cancers

摘要

The tubulin polymerization is an attractive target for anticancer therapy and in the development of cancer imaging agents for use in biomedical imaging technique positron emission tomography (PET). 7-Aroyl-aminoindoline-1-sulfonamides are a novel class of potent antitublin agents. Carbon-11-labeled 7-aroyl-aminoindoline-1-sulfonamides have been synthesized as new potential PET agents for imaging of tubulin polymerization in cancers. The target tracers were prepared by 0-[~(11)C]methylation of their corresponding precursors using [~(11)C]CH_3OTf and isolated by a simplified solid-phase extraction purification procedure in 40-55% radiochemical yields based on [~(11)C]CO_2 and decay corrected to the end of bombardment (EOB), 15-20 min overall synthesis time from EOB, >98% radiochemical purity, and 74-111 GBq/mumol specific activity at the end of synthesis.