1-(β-D-lyxofuranosyl)thymine | 4348-54-3

• 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-(β-D-lyxofuranosyl)thymine
• 英文别名: β-D-lyxothymine；1-β-D-Lyxofuranosyl-thymin；1-β-D-lyxofuranosyl-5-methyl-1H-pyrimidine-2,4-dione；1-β-D-Lyxofuranosyl-5-methyl-1H-pyrimidin-2,4-dion；1-(b-D-Arabinofuranosyl)thymine；1-[(2R,3S,4R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione
• CAS: 4348-54-3
• 化学式: C₁₀H₁₄N₂O₆
• 分子量: 258.231
• InChiKey: DWRXFEITVBNRMK-UTSKPXGSSA-N

物化性质

• 熔点：
  186-187.5 °C(Solv: ethanol (64-17-5))
• 密度：
  1.576±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  119
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  Diethyl-phosphoramidous acid (2R,3R,4S,5R)-5-(6-benzoylamino-purin-9-yl)-2-[bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-4-hydroxy-tetrahydro-furan-3-yl ester 2-cyano-1,1-dimethyl-ethyl ester 、 1-(β-D-lyxofuranosyl)thymine 在 四氮唑 、 叔丁基过氧化氢 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  （2-氰基-1,1-二甲基乙氧基）双（二乙基氨基）膦：合成DNA片段的方便试剂

  摘要：

  磷酸化试剂（2-氰基-1,1-二甲基乙氧基）双（二乙基氨基）膦被证明对于原位制备d-核苷亚磷酰胺非常有效。后面的这些化合物可用于引入3'，5'-核苷酸间键并用于在溶液中和在固体支持物上合成DNA片段。通过氨解很容易实现P（V）上2-氰基-1,1-二甲基乙基保护基的去除。

  DOI：

  10.1002/recl.19871060302
• 作为产物：
  描述：

  1-(β-D-xylofuranosyl)-thymine 在 吡啶 、 二氯乙酸 、 sodium tetrahydroborate 、 四丁基氟化铵 、 二甲基亚砜 、 N,N'-二环己基碳二亚胺 作用下， 以 四氢呋喃 、 乙醇 、 苯 为溶剂， 反应 6.0h， 生成 1-(β-D-lyxofuranosyl)thymine
  参考文献：
  名称：

  五个天然存在的核酸碱基的α-和β-D-呋喃糖基核苷的系统合成和生物学评估。

  摘要：

  天然存在的核苷的α-和β-D-呋喃呋喃糖基类似物已经合成，并检查了它们的抗病毒特性。通过将嘌呤和嘧啶糖苷配基与四-O-乙酰基-α-D-lyxofurananose糖基化，然后除去保护基团来制备α端基异构体。通过依次氧化和还原3'，5'-O-（1,1,3,3-四异丙基二硅氧烷-1,3-二基）-β-Dx呋喃呋喃糖基核苷来获得β端基异构体。测试了呋喃呋喃糖基核苷对多种RNA和DNA病毒的活性以及对细胞生长的抑制作用。一种化合物9-α-D-lyxofuranosyladenine在体外和体内均显示出对1型和2型单纯疱疹病毒的活性。

  DOI：

  10.1021/jm00389a005

文献信息

• TREATMENT INVOLVING INTERLEUKIN-2 (IL2) AND INTERFERON (IFN)
  申请人：BIONTECH SE

  公开号：US20220143144A1

  公开（公告）日：2022-05-12

  The present disclosure relates to methods and agents for enhancing the effect of immune effector cells, in particular immune effector cells that respond to interleukin-2 (IL2), for example effector T cells such as CD8+ T cells. Specifically, the present disclosure relates to methods comprising administering to a subject a polypeptide comprising IL2 or a functional variant thereof or a polynucleotide encoding a polypeptide comprising IL2 or a functional variant thereof and a polypeptide comprising type I interferon (IFN) or a functional variant thereof or a polynucleotide encoding a polypeptide comprising type I interferon or a functional variant thereof.

  本公开涉及增强免疫效应细胞的方法和药剂，特别是对介白质-2（IL2）作出反应的免疫效应细胞，例如效应T细胞（如CD8+ T细胞）。具体而言，本公开涉及的方法包括向受试者给予包含IL2或其功能变体的多肽或编码包含IL2或其功能变体的多肽的多核苷酸和包含I型干扰素（IFN）或其功能变体的多肽或编码包含I型干扰素或其功能变体的多肽的多核苷酸。
• Profiling chemically modified DNA/RNA units for disease and cancer diagnosis
  申请人：The Research Foundation for The State University of New York

  公开号：US11339441B2

  公开（公告）日：2022-05-24

  The present invention relates to high-throughput methods comprising direct infusion electrospray ionization mass spectrometry (ESI-MS), multistep tandem mass spectrometry (MSn), consecutive reaction monitoring (CRM), ion mobility spectrometry mass spectrometry (IMS-MS), high-resolution MS, and IMS-MS, for genome-wide (whole cell or tissue) profiling of DNA and RNA nucleotides/nucleosides having a wide variety of variant structural modifications. In particular, these methods are contemplated for providing a specific profile of variant DNA and/or RNA chemically modified nucleic acids (i.e. structures) associated with specific medical conditions. Medical conditions may include, but are not limited to: cancer; including prostate, lung, uterus, larynx, ovary, breast, kidney, and many other types of cancers; specific stages of cancer; bacterial infections; viral infections; genetic and metabolic disorders; and any condition involving changes in DNA and/or RNA structural modifications.

  本发明涉及高通量方法，包括直接注入电喷雾离子化质谱（ESI-MS）、多步串联质谱（MSn）、连续反应监测（CRM）、离子迁移谱质谱（IMS-MS）、高分辨率 MS 和 IMS-MS，用于对具有多种变异结构修饰的 DNA 和 RNA 核苷酸/核苷进行全基因组（全细胞或组织）分析。特别是，这些方法可用于提供与特定病症相关的变异 DNA 和/或 RNA 化学修饰核酸（即结构）的特定概况。病症可包括但不限于：癌症；包括前列腺癌、肺癌、子宫癌、喉癌、卵巢癌、乳腺癌、肾癌和许多其他类型的癌症；癌症的特定阶段；细菌感染；病毒感染；遗传和代谢紊乱；以及任何涉及 DNA 和/或 RNA 结构修饰变化的病症。
• Pyrimidine Nucleosides. IV. The Synthesis of 1-β-D-Lyxofuranosylthymine¹
  作者：Jack J. Fox、John F. Codington、Naishun C. Yung、Louis Kaplan、J. O. Lampen

  DOI：10.1021/ja01552a036

  日期：1958.10
• PROFILING CHEMICALLY MODIFIED DNA/RNA UNITS FOR DISEASE AND CANCER DIAGNOSIS
  申请人：THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK

  公开号：US20170044619A1

  公开（公告）日：2017-02-16

  The present invention relates to high-throughput methods comprising direct infusion electrospray ionization mass spectrometry (ESI-MS), multistep tandem mass spectrometry (MS n ), consecutive reaction monitoring (CRM), ion mobility spectrometry mass spectrometry (IMS-MS), high-resolution MS, and IMS-MS, for genome-wide (whole cell or tissue) profiling of DNA and RNA nucleotides/nucleosides having a wide variety of variant structural modifications. In particular, these methods are contemplated for providing a specific profile of variant DNA and/or RNA chemically modified nucleic acids (i.e. structures) associated with specific medical conditions. Medical conditions may include, but are not limited to: cancer; including prostate, lung, uterus, larynx, ovary, breast, kidney, and many other types of cancers; specific stages of cancer; bacterial infections; viral infections; genetic and metabolic disorders; and any condition involving changes in DNA and/or RNA structural modifications.
• Treatment Involving Therapeutic Antibody and Interleukin-2 (IL2)
  申请人：BioNTech SE

  公开号：US20220378876A1

  公开（公告）日：2022-12-01

  Tumor cells often evade an immune response, e.g., by reducing or eliminating MHC expression and/or IFN-signaling, which enables uncontrolled growth. We demonstrate herein that antibody-based immunotherapy in combination with IL2 administration is an effective therapy against such resistant tumors. Specifically, the present disclosure relates to methods of treating a subject with cancer that is at least partially resistant to an MHC-dependent T cell response comprising administering to the subject: a. a polypeptide comprising IL2 or a functional variant thereof or a polynucleotide encoding a polypeptide comprising IL2 or a functional variant thereof; and b. antibody-based immunotherapy.