کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1378774 | 982009 | 2005 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: A novel [99mTcN]2+ complex of metronidazole xanthate as a potential agent for targeting hypoxia A novel [99mTcN]2+ complex of metronidazole xanthate as a potential agent for targeting hypoxia](/preview/png/1378774.png)
A xanthate derivative (L) at the pendant hydroxy group of metronidazole, a nitroimidazole known to possess affinity for hypoxic tumors, has been used as the carrier molecule for targeted delivery of the gamma-emitting radioisotope 99mTc to tumors. The xanthate residues (S2−) from two molecules of this ligand (L) were used for chelation with the [99mTcN]2+ intermediate to form a square pyramidal and neutral [99mTcN/L2] complex in >95% yield using a low ligand concentration of 1 mg/mL (∼3 × 10−3 M). Biodistribution studies carried out in Swiss mice bearing fibrosarcoma tumor showed selective accumulation of the injected activity in the tumor (1.44 ± 0.26% per gram 1 h pi) with major clearance through hepatobiliary route. The complex showed high tumor/muscle ratio (2.15 and 3.35 at 1 and 3 h post-injection, respectively) and tumor/blood ratio, which were comparable to hypoxia targeting agents 99mTc-BMS181321 and 99mTc-BRU59-21 reported earlier.
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 14, 15 July 2005, Pages 3398–3401