Synthesis and preliminary evaluation of novel (99m)Tc-labeled folate derivative via click reaction for SPECT imaging

Zhide Guo; Pu Zhang; Manli Song; Xiaowei Wu; Chang Liu; Zuoquan Zhao; Jie Lu; Xianzhong Zhang

doi:10.1016/j.apradiso.2014.04.020

Synthesis and preliminary evaluation of novel (99m)Tc-labeled folate derivative via click reaction for SPECT imaging

Appl Radiat Isot. 2014 Sep:91:24-30. doi: 10.1016/j.apradiso.2014.04.020. Epub 2014 May 14.

Authors

Zhide Guo¹, Pu Zhang², Manli Song³, Xiaowei Wu³, Chang Liu², Zuoquan Zhao², Jie Lu⁴, Xianzhong Zhang⁵

Affiliations

¹ Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, 19 Xinjiekou Outer Street, Beijing 100875, China. Electronic address: guozhide0518@gmail.com.
² Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, 19 Xinjiekou Outer Street, Beijing 100875, China; Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiang׳an South Road, Xiamen 361102, China.
³ Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiang׳an South Road, Xiamen 361102, China.
⁴ Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, 19 Xinjiekou Outer Street, Beijing 100875, China.
⁵ Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiang׳an South Road, Xiamen 361102, China. Electronic address: zhangxzh@xmu.edu.cn.

PMID: 24880914
DOI: 10.1016/j.apradiso.2014.04.020

Abstract

The folate receptor is over expressed in a wide variety of human tumors. In this study, a novel (99m)Tc-labeled folate derivative ((99m)Tc-HYNIC-T-FA) was synthesized as a potential FR-targeting imaging probe and its efficiency was evaluated. This (99m)Tc-complex could be obtained through practical manner and showed improved in vivo characteristics compared with other radiofolates. Thus, this novel (99m)Tc-HYNIC-T-FA compound could serve as a potential imaging agent for folate receptor positive tumors.

Keywords: (99m)Tc-labeled folate derivatives; Click chemistry; Folate receptor; KB tumor; SPECT/CT.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Carcinoma
Cell Line, Tumor
Click Chemistry
Female
Folic Acid / analogs & derivatives*
Folic Acid / chemistry
Humans
Magnetic Resonance Spectroscopy
Mice
Mice, Nude
Nasopharyngeal Carcinoma
Nasopharyngeal Neoplasms / diagnosis*
Organotechnetium Compounds / chemical synthesis*
Organotechnetium Compounds / chemistry
Radiopharmaceuticals / chemical synthesis*
Radiopharmaceuticals / chemistry
Spectrometry, Mass, Electrospray Ionization
Tomography, Emission-Computed, Single-Photon / methods
Xenograft Model Antitumor Assays

Substances

Organotechnetium Compounds
Radiopharmaceuticals
Folic Acid