کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10593116 | 981804 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Effect of a second nitroimidazole redox centre on the accumulation of a hypoxia marker: Synthesis and in vitro evaluation of 99mTc-labeled bisnitroimidazole propylene amine oxime complexes
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Up to now, most of the hypoxia markers contain only one nitroimidazole redox centre, such as Oxo[[3,3,9,9-tetramethyl-1-(2-nitro-1H-imidazol-1-yl)-4,8-diazaundecane-2,10-dione dioximato] (3-)-N,Nâ²,Nâ³,Nâ³â²]-technetium (99mTc-1, BMS181321). Introducing a second nitroimidazole redox centre may enhance the hypoxic accumulation of the markers. In the present work, four 99mTc-1 (BMS181321, containing one 2-nitroimidazole) analogues, that is, 99mTc-2 (containing two 2-nitroimidazoles), 99mTc-3 (containing one 4-nitroimidazole), 99mTc-4 (containing two 4-nitroimidazoles) and 99mTc-5 (containing both a 2-nitroimidazole and a 4-nitroimidazole) were synthesized, and the hypoxic accumulation was evaluated in vitro using murine sarcoma S180 cells. 99mTc-3 and 99mTc-4 displayed no significant anoxic/normoxic differentials, whereas 99mTc-1 (BMS181321), 99mTc-2 and 99mTc-5 showed high anoxic cellular uptakes. The anoxic uptake of 99mTc-2 reached up to 59.0 ± 0.9% at 4 h, which was 2.4 times as that of 99mTc-1. 99mTc-2 displayed high hypoxic accumulation, indicating that introducing a second nitroimidazole redox centre, that is, 2-nitroimidazole, affected the hypoxic accumulation. Consequently, 99mTc-2 may serve as a viable candidate for hypoxia marker. This finding may eventually lead to the development of compounds containing multi-redox centres as hypoxia markers.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 1, 1 January 2012, Pages 172-177
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 1, 1 January 2012, Pages 172-177
نویسندگان
Huafan Huang, Hao Zhou, Zejun Li, Xiangyun Wang, Taiwei Chu,