Citation: Jin Ming Zhang, Xiao Jun Zhang, Zhi Hong Xu, Jia He Tian. Radiosynthesis of N-¹¹C-meisoindigotin as a novel PET agent for imaging of cyclin-dependent kinases and GSK-3β[J]. Chinese Chemical Letters, ;2012, 23(2): 205-207. doi: 10.1016/j.cclet.2011.10.014 shu

Radiosynthesis of N-¹¹C-meisoindigotin as a novel PET agent for imaging of cyclin-dependent kinases and GSK-3β

a Department of Nuclear Medicine, The PLA General Hospital, Beijing 100853, China;
b Huayi Chemicals Co., Ltd., Changshu 215522, China

Received Date: 1 July 2011

Fund Project: This work was supported by grants from the National Natural Science Foundation of China (No. 81071170).

Meisoindigotin has been demonstrated as a new type of cancer chemotherapeutic agent. N-11C-Meisoindigotin was synthesized by N-¹¹C-methylation of the isoindigotin precursor with ¹¹C-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-¹¹C]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-¹¹C-Meisoindigotin was a promising candidate for further development as a novel PET radiotracer for imaging of cyclin-dependent kinases (CDKs) and GSK-3β.
- N-Methylisoindigotin,
- Tumor imaging agent,
- Cyclin-dependent kinases
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