Novel 99mTc labeled complexes with bisphosphonate isocyanide: Radiosynthesis and evaluation as potential bone-seeking agents

Di Xiao; Yuhao Jiang; Junhong Feng; Qing Ruan; Qianna Wang; Guangxing Yin; Junbo Zhang

doi:10.1016/j.bmcl.2022.128918

Novel ^99mTc labeled complexes with bisphosphonate isocyanide: Radiosynthesis and evaluation as potential bone-seeking agents

Bioorg Med Chem Lett. 2022 Oct 1:73:128918. doi: 10.1016/j.bmcl.2022.128918. Epub 2022 Aug 1.

Authors

Di Xiao¹, Yuhao Jiang¹, Junhong Feng¹, Qing Ruan¹, Qianna Wang¹, Guangxing Yin¹, Junbo Zhang²

Affiliations

¹ Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
² Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, PR China. Electronic address: zhjunbo@bnu.edu.cn.

PMID: 35926798
DOI: 10.1016/j.bmcl.2022.128918

Abstract

In order to develop ^99mTc-labeled complexes with bisphosphonate isocyanide as novel bone imaging agents, two bisphosphonate isocyanide derivatives (CNALN and CNPAM) were synthesized and radiolabeling was performed for preparing the corresponding [^99mTc]Tc(I) complexes. [^99mTc]Tc-CNALN and [^99mTc]Tc-CNPAM were obtained with high radiochemical purity and showed good in vitro stability. Both of them were hydrophilic and had high affinity to hydroxyapatite. The biodistribution studies in mice revealed [^99mTc]Tc-CNALN showed higher bone/background ratios at 60 min post-injection. In single photon emission computed tomography (SPECT) imaging study, [^99mTc]Tc-CNALN had an obvious accumulation in bone, suggesting it would be a promising bone-seeking agent.

Keywords: Alendronate; Bone imaging; Isocyanide; Pamidronate; Technetium-99m.

Publication types

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

MeSH terms

Animals
Cyanides
Diphosphonates* / chemistry
Mice
Organotechnetium Compounds* / chemistry
Radiopharmaceuticals / pharmacology
Technetium / chemistry
Tissue Distribution
Tomography, Emission-Computed, Single-Photon / methods

Substances

Cyanides
Diphosphonates
Organotechnetium Compounds
Radiopharmaceuticals
Technetium