Meisoindigotin has been demonstrated as a new type of cancer chemotherapeutic agent.N-^(11)C-meisoindigotin was synthesized by N-^(11)C-methyIation of the isoindigotin precursor with ^(11)C-labelled methyl trifl...Meisoindigotin has been demonstrated as a new type of cancer chemotherapeutic agent.N-^(11)C-meisoindigotin was synthesized by N-^(11)C-methyIation of the isoindigotin precursor with ^(11)C-labelled methyl triflate.The decay corrected radiochemical yields were 15-25%,and the specific radioactivity was 1.0-1.2 Ci/μmol at the end of synthesis.The cellular uptake of[N-^(11)C]-meisoindigotin was evaluated in four different lung cancer cell lines.Our results showed that the A549,GLC-82,95D cell lines exhibited higher uptake than 95C cell line after incubation for 60 min.N-^(11)-meisoindigotin was a promising candidate for further development as a novel PET radiotracer for imaging of cyclin-dependent kinases(CDKs) and GSK-3β.展开更多
基金supported by grants from the National Natural Science Foundation of China(No81071170)
文摘Meisoindigotin has been demonstrated as a new type of cancer chemotherapeutic agent.N-^(11)C-meisoindigotin was synthesized by N-^(11)C-methyIation of the isoindigotin precursor with ^(11)C-labelled methyl triflate.The decay corrected radiochemical yields were 15-25%,and the specific radioactivity was 1.0-1.2 Ci/μmol at the end of synthesis.The cellular uptake of[N-^(11)C]-meisoindigotin was evaluated in four different lung cancer cell lines.Our results showed that the A549,GLC-82,95D cell lines exhibited higher uptake than 95C cell line after incubation for 60 min.N-^(11)-meisoindigotin was a promising candidate for further development as a novel PET radiotracer for imaging of cyclin-dependent kinases(CDKs) and GSK-3β.