fac-(99m)Tc(CO)3(([10-(10-([5-Et-2'5'-dideoxyuridine-5'-Me]carbamoyl)decylcarbamoyl)decyl]methoxycarbonylmethyl-amino)acetato)(1- | 933448-45-4

• 英文名称: fac-(99m)Tc(CO)3(([10-(10-([5-Et-2'5'-dideoxyuridine-5'-Me]carbamoyl)decylcarbamoyl)decyl]methoxycarbonylmethyl-amino)acetato)(1-
• CAS: 933448-45-4
• 化学式: C₄₀H₆₁N₅O₁₃Tc
• 分子量: 918.95
• InChiKey: WHEKPAWFUIOXNZ-CRGIYFQLSA-L

反应信息

• 作为产物：
  描述：

  fac-triaquatricarbonyltechnetium-99m(1+) 、 ([10-(10-([5-ethyl-2',5'-dideoxyuridine-5'-methyl]carbamoyl)-decylcarbamoyl)-decyl]-methoxycarbonylmethyl-amino)-acetic acid hydrate 以 水 、 二甲基亚砜 为溶剂， 生成 fac-(99m)Tc(CO)3(([10-(10-([5-Et-2'5'-dideoxyuridine-5'-Me]carbamoyl)decylcarbamoyl)decyl]methoxycarbonylmethyl-amino)acetato)(1-
  参考文献：
  名称：

  Synthesis of tricarbonyl rhenium and technetium complexes of a 5′-carboxamide 5-ethyl-2′-deoxyuridine for selective inhibition of herpes simplex virus thymidine kinase 1

  摘要：

  Herpes simplex virus thymidine kinase type 1 (HSV1-TK) is frequently used as reporter protein in gene therapy. Our aim is to produce single photon emitting reporter probe based on technetium-99m. The synthesis of organometallic technetium and rhenium complexes of a 5'-carboxamide 5-ethyl-2'-deoxyuridine derivative able to selectively inhibit HSV1-TK is presented. The 5-ethyl-2'-deoxyuridine functionalized with a suitable tridentate chelating system at position 5' was synthesized from commercial 2'-deoxyuridine in seven steps. The 5-ethyl-2'-deoxyuridine derivative was labeled with the fac-M(CO)(3)-core (M = Tc, Re). The resulting rhenium complex was found to be a selective competitive inhibitor of HSV1-TK (K-i = 4.56 mu M). Inhibition of the human cytosolic thymidine kinase (hTK1) previously reported with organometallic rhenium and technetium complexes of 5'-carboxamide thymidine derivative was not observed. The uptake of the technetium-99m complex in transfected cells expressing HSV1-TK has been evaluated to assess its possible use as reporter. (C) 2006 Elsevier B.V. All rights reserved.

  DOI：

  10.1016/j.jorganchem.2006.10.011