Synthesis and preliminary biological evaluation of the 99mTc labeled nitrobenzoimidazole and nitrotriazole as tumor hypoxia markers.
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.
Zhang
Yu
Y
Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Chu
Taiwei
T
Gao
Xuguang
X
Liu
Xinqi
X
Yang
Zhi
Z
Guo
Zhenquan
Z
Wang
Xiangyun
X
D000577:Amides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D014408:Biomarkers, Tumor / Q000032:analysis*; D045744:Cell Line, Tumor; D007093:Imidazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051379:Mice; D015609:Organotechnetium Compounds / Q000737:chemistry*; D020005:Propanols / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
C511813:1-(3-1,2,4-nitrotriazole-1-yl)-propanhydroxyiminoamide; C511814:1-(6-nitrobenzoimidazole-1-yl)-propanhydroxyiminoamide; D000577:Amides; D014408:Biomarkers, Tumor; D007093:Imidazoles; D015609:Organotechnetium Compounds; D020005:Propanols; D014230:Triazoles