1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-5-propyl-pyrimidine-2,4-dione

• 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: 1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-5-propyl-pyrimidine-2,4-dione
• 英文别名: 1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-propylpyrimidine-2,4-dione
• 化学式: C₁₂H₁₈N₂O₆
• 分子量: 286.28
• InChiKey: QOYQGDIJMBALFN-SDNRWEOFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  119
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• Novel entities for cancer therapy
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP0415731A2

  公开（公告）日：1991-03-06

  Novel molecular chimaeras produced by recombinant DNA techniques are described. They comprise a target tissue specific transcriptional regulatory sequence (TRS) linked and controlling the expression of a heterologous enzyme for example Varicella Zoster Virus Thymidine Kinase (VZV TK) gene. A molecular chimaera is packaged into a synthetic retroviral particle which is capable of infecting mammalian tissue. This in turn may be administered to a patient, and the TRS will be selectively transcriptionally activated in the target tissue (for example cancerous tissue). Administration of compounds which are selectively metabolised by the enzyme produce cytotoxic or cytostatic metabolites in situ thereby selectively killing or arresting the growth of the target cell.

  本文描述了通过 DNA 重组技术生产的新型分子嵌合体。它们包括一个目标组织特异性转录调控序列（TRS），该序列连接并控制异源酶的表达，例如水痘带状疱疹病毒胸苷激酶（VZV TK）基因。分子嵌合体被包装成能够感染哺乳动物组织的合成逆转录病毒颗粒。然后将其注射给病人，TRS 将在目标组织（例如癌组织）中被选择性地转录激活。施用经该酶选择性代谢的化合物，可在原位产生细胞毒性或细胞抑制性代谢产物，从而选择性地杀死或抑制靶细胞的生长。
• METHOTREXATE ADJUVANTS TO REDUCE TOXICITY AND METHODS FOR USING THE SAME
  申请人：Tosk, Inc.

  公开号：EP2265274A2

  公开（公告）日：2010-12-29
• JPH04253914A
  申请人：——

  公开号：JPH04253914A

  公开（公告）日：1992-09-09
• US5028596A
  申请人：——

  公开号：US5028596A

  公开（公告）日：1991-07-02
• [EN] METHOTREXATE ADJUVANTS TO REDUCE TOXICITY AND METHODS FOR USING THE SAME<br/>[FR] ADJUVANTS POUR RÉDUIRE LA TOXICITÉ DU MÉTHOTREXATE, ET PROCÉDÉS D'UTILISATION
  申请人：TOSK INC

  公开号：WO2009114325A2

  公开（公告）日：2009-09-17

  Methods are provided for using methotrexate (MTX) active agents in which reduced host toxicity is observed. Aspects of the methods include administering to a subject an effective amount of an MTX active agent in conjunction with a MTX toxicity-reducing adjuvant, such as a 2,2'-anhydropyrimidine, a derivative thereof or a uridine phosphorylase inhibitor. Also provided are compositions and kits that find use in practicing embodiments of the invention. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.