Synthesis and preliminary biological evaluation of the 99mTc labeled nitrobenzoimidazole and nitrotriazole as tumor hypoxia markers

Yu Zhang; Taiwei Chu; Xuguang Gao; Xinqi Liu; Zhi Yang; Zhenquan Guo; Xiangyun Wang

doi:10.1016/j.bmcl.2006.01.001

Synthesis and preliminary biological evaluation of the 99mTc labeled nitrobenzoimidazole and nitrotriazole as tumor hypoxia markers

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1831-3. doi: 10.1016/j.bmcl.2006.01.001. Epub 2006 Feb 7.

Authors

Yu Zhang¹, Taiwei Chu, Xuguang Gao, Xinqi Liu, Zhi Yang, Zhenquan Guo, Xiangyun Wang

Affiliation

¹ Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.

PMID: 16460938
DOI: 10.1016/j.bmcl.2006.01.001

Abstract

1-(3-1,2,4-Nitrotriazole-1-yl)-propanhydroxyiminoamide and 1-(6-nitrobenzoimidazole-1-yl)-propanhydroxyiminoamide were synthesized and radiolabeled with (99m)Tc. The (99m)Tc labeled complexes continuously accumulated in hypoxic murine sarcoma S180 cells in vitro but not in aerobic cells. Biodistribution results in mice bearing S180 tumor indicated that the tracers could localize in tumor and eliminate from it slowly. These results suggested that the (99m)Tc labeled nitrobenzoimidazole and nitrotriazole might be the novel tumor hypoxia markers.

Publication types

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

MeSH terms

Amides / chemical synthesis*
Amides / pharmacokinetics
Amides / pharmacology
Animals
Biomarkers, Tumor / analysis*
Cell Line, Tumor
Imidazoles / chemical synthesis*
Imidazoles / pharmacokinetics
Imidazoles / pharmacology
Mice
Organotechnetium Compounds / chemistry*
Propanols / chemical synthesis*
Propanols / pharmacokinetics
Propanols / pharmacology
Triazoles / chemical synthesis*
Triazoles / pharmacokinetics
Triazoles / pharmacology

Substances

1-(3-1,2,4-nitrotriazole-1-yl)-propanhydroxyiminoamide
1-(6-nitrobenzoimidazole-1-yl)-propanhydroxyiminoamide
Amides
Biomarkers, Tumor
Imidazoles
Organotechnetium Compounds
Propanols
Triazoles