5-carbamoyl-2'-deoxyuridine | 110914-09-5

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘧啶核苷
• 英文名称: 5-carbamoyl-2'-deoxyuridine
• 英文别名: 1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-2,4-dioxo-pyrimidine-5-carboxamide；1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2,4-dioxopyrimidine-5-carboxamide
• CAS: 110914-09-5
• 化学式: C₁₀H₁₃N₃O₆
• 分子量: 271.23
• InChiKey: BOFVRFUMKYMSBC-RRKCRQDMSA-N

物化性质

• 密度：
  1.641±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.9
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  142
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  5-carbamoyl-2'-deoxyuridine 在 吡啶 、 silica gel 作用下， 反应 4.0h， 生成 5-carbamoyl-3'-(4-chlorophenyl)phosphate-2'-deoxy-5'-O-(4,4'-dimethoxytrityl)-uridine triethylammonium salt
  参考文献：
  名称：

  Fukuda, Tsunehiko; Hamana, Takumi; Kikuchi, Kaeko, Zeitschrift fur Naturforschung, Teil B: Anorganische Chemie, Organische Chemie, 1986, vol. 41, # 12, p. 1571 - 1579

  摘要：

  DOI：
• 作为产物：
  描述：

  四乙酰核糖 在 吡啶 、 4-二甲氨基吡啶 、 ammonium hydroxide 、 三甲基氯硅烷 、 偶氮二异丁腈 、 四丁基氟化铵 、 三正丁基氢锡 、 四氯化锡 、 六甲基二硅氮烷 作用下， 以 1,4-二氧六环 、 吡啶 、 二氯甲烷 、 乙腈 为溶剂， 反应 59.5h， 生成 5-carbamoyl-2'-deoxyuridine
  参考文献：
  名称：

  Fukuda, Tsunehiko; Hamana, Takumi; Kikuchi, Kaeko, Zeitschrift fur Naturforschung, Teil B: Anorganische Chemie, Organische Chemie, 1986, vol. 41, # 12, p. 1571 - 1579

  摘要：

  DOI：

文献信息

• Post-selec modification methods
  申请人：SomaLogic, Inc.

  公开号：US10221421B2

  公开（公告）日：2019-03-05

  Aptamers that bind PDGF and aptamers that bind VEGF are provided. In addition, aptamer constructs comprising a PDGF aptamer and a VEGF aptamer are provided. Pharmaceutical compositions comprising the aptamers and aptamer constructs are provided, as well as methods of treating conditions using the aptamers and aptamer constructs.

  本研究提供了结合 PDGF 的适配体和结合 VEGF 的适配体。此外，还提供了包含 PDGF 拟合物和 VEGF 拟合物的拟合物构建体。本研究还提供了包含该适配体和适配体构建体的药物组合物，以及使用该适配体和适配体构建体治疗疾病的方法。
• PDGF and VEGF aptamers having improved stability and their use in treating PDGF and VEGF mediated diseases and disorders
  申请人：SomaLogic, Inc.

  公开号：US10544419B2

  公开（公告）日：2020-01-28

  Aptamers having improved stability against nucleases that bind PDGF and aptamers that bind VEGF are provided. In addition, aptamer constructs comprising a PDGF aptamer and a VEGF aptamer are provided. Pharmaceutical compositions comprising the aptamers and aptamer constructs are provided, as well as methods of treating conditions using the aptamers and aptamer constructs.

  本研究提供了对结合 PDGF 的核酸酶和结合 VEGF 的适配体具有更高抗稳定性的适配体。此外，还提供了包含 PDGF 拟合物和 VEGF 拟合物的拟合物构建体。本发明还提供了包含该适配体和适配体构建体的药物组合物，以及使用该适配体和适配体构建体治疗疾病的方法。
• Post-selex modification methods
  申请人：SomaLogic, Inc.

  公开号：US11208663B2

  公开（公告）日：2021-12-28

  Aptamers that bind PDGF and aptamers that bind VEGF are provided. In addition, aptamer constructs comprising a PDGF aptamer and a VEGF aptamer are provided. Pharmaceutical compositions comprising the aptamers and aptamer constructs are provided, as well as methods of treating conditions using the aptamers and aptamer constructs.

  本研究提供了结合 PDGF 的适配体和结合 VEGF 的适配体。此外，还提供了包含 PDGF 拟合物和 VEGF 拟合物的拟合物构建体。本研究还提供了包含该适配体和适配体构建体的药物组合物，以及使用该适配体和适配体构建体治疗疾病的方法。
• 5-Modified-2′-dU and 2′-dC as Mutagenic Anti HIV-1 Proliferation Agents: Synthesis and Activity
  作者：Yazan El Safadi、Jean-Christophe Paillart、Géraldine Laumond、Anne-Marie Aubertin、Alain Burger、Roland Marquet、Valérie Vivet-Boudou

  DOI：10.1021/jm901758f

  日期：2010.2.25

  With the goal of limiting HIV-1 proliferation by increasing the mutation rate of the viral genome, we synthesized a series of pyrimidine nucleoside analogues modified in position 5 of the aglycone moiety but unmodified oil the sugar part. The synthetic strategies allow us to prepare the targeted compounds directly from commercially available nucleosides. All compounds were tested for their ability to reduce HIV-1 Proliferation in cell culture. Two of them (5-hydroxymethyl-2'-dU (1c) and 5-hydroxymethyl-2'-dC (2c)) displayed a moderate antiviral activity in single passage experiments. The same two compounds Plus two additional ones (5-carbamoyl-2'-dU (1a) and 5-carbamoylmethyl-2'-dU(1b)) were potent inhibitors of HIV-1 RT activity in serial passage assays, in which they induced a progressive loss of HIV-1 replication. In addition, viruses collected after seven passages in the presence of 1c and 2c replicated very poorly after withdrawal of these compounds, consistent with the accumulation of deleterious mutations in the HIV-1 genome.
• APTAMERS TO PDGF AND VEGF AND THEIR USE IN TREATING PDGF AND VEGF MEDIATED CONDITIONS
  申请人：Somalogic, Inc.

  公开号：EP2831278A1

  公开（公告）日：2015-02-04