5-氟尿苷-5-o-b-d-半乳糖吡喃糖苷 | 149965-92-4

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘧啶核苷
• 中文名称: 5-氟尿苷-5-o-b-d-半乳糖吡喃糖苷
• 英文名称: 5-fluorouridine-5'-O-β-D-galactopyranoside
• 英文别名: 5-fluoro-5'-O-(β-D-galactopyranosyl)uridine；5-fluorouridine-5’-O-β-D-galactopyranoside；5-FUR-β-gal；5'-O-beta-D-Galactosyl-5-fluorouridine；1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]oxolan-2-yl]-5-fluoropyrimidine-2,4-dione
• CAS: 149965-92-4
• 化学式: C₁₅H₂₁FN₂O₁₁
• 分子量: 424.337
• InChiKey: BTPARJRXLUUYJW-FQKYAJAOSA-N

物化性质

• 密度：
  1.81±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -4.1
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.73
• 拓扑面积：
  199
• 氢给体数：
  7
• 氢受体数：
  12

反应信息

• 作为产物：
  描述：

  5-fluorouridine-5'-O-β-D-galactopyranoside peracetate 在 sodium methylate 作用下， 以 甲醇 为溶剂， 反应 18.0h， 以87%的产率得到5-氟尿苷-5-o-b-d-半乳糖吡喃糖苷
  参考文献：
  名称：

  Compositions and methods for targeted enzymatic release of cell regulatory compounds

  摘要：

  本发明描述了新型前药及其用于改变活细胞、组织或整个生物体的生长和生物学特性的方法。该方法允许在表达激活前药酶基因的转化宿主细胞附近或附近选择性地激活前药。根据本发明的一个优选实施例，前药是生物活性化合物与能够通过酶作用从生物活性化合物中裂解出来的化学基团的缀合物。根据本发明的方法包括：(a)将编码酶的基因引入目标细胞；(b)施用前药，其中酶从前药缀合物中释放前药。在本发明的一个优选实施例中，编码酶的基因是标记基因。

  公开号：

  US06656917B1

文献信息

• Synthesis of Disaccharide Nucleosides Utilizing the Temporary Protection of the 2′,3′-cis-Diol of Ribonucleosides by a Boronic Ester
  作者：Hidehisa Someya、Taiki Itoh、Shin Aoki

  DOI：10.3390/molecules22101650

  日期：——

  activities. In this study, we report on the synthesis of disaccharide nucleosides utilizing the temporary protection of the 2',3'-cis-diol of ribonucleosides, such as adenosine, guanosine, uridine, 5-metyluridine, 5-fluorouridine and cytidine, by a boronic ester. The temporary protection of the above ribonucleosides permits the regioselective O-glycosylation of the 5'-hydroxyl group with thioglycosides using

  二糖核苷是一类重要的天然化合物，具有多种生物活性。在这项研究中，我们报道了利用核糖核苷（如腺苷、鸟苷、尿苷、5-甲基尿苷、5-氟尿苷和胞苷）的2',3'-顺式二醇的临时保护来合成二糖核苷，通过硼酸酯。上述核糖核苷的临时保护允许使用对甲苯磺酰氯（p-TolSCl）/三氟甲磺酸银（AgOTf）启动子系统将5'-羟基与硫代糖苷进行区域选择性O-糖基化，以相当好的方式提供相应的二糖核苷。化学产率。通过 1 H、 11B 和 19 F NMR 光谱检查由尿苷和 4-（三氟甲基）苯基硼酸制备的硼酸酯的形成。
• Polypeptides and nucleic acids encoding the same
  申请人：GENENTECH, INC.

  公开号：EP1659131A2

  公开（公告）日：2006-05-24

  The present invention is directed to novel polypeptides and to nucleic acid molecules encoding those polypeptides. Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention.

  本发明涉及新型多肽和编码这些多肽的核酸分子。本发明还提供了包含这些核酸序列的载体和宿主细胞、包含与异源多肽序列融合的本发明多肽的嵌合多肽分子、与本发明多肽结合的抗体以及生产本发明多肽的方法。
• Senolytic compositions and uses thereof
  申请人：Rubedo Life Sciences, Inc.

  公开号：US11026963B2

  公开（公告）日：2021-06-08

  Provided herein are senolytic agents for selectively killing senescent cells that are associated with numerous pathologies and diseases, including age-related pathologies and diseases. As disclosed herein, senescent cell-associated diseases and disorders may be treated or prevented by administering at least one senolytic agent or pharmaceutical compositions thereof. The senescent cell-associated diseases or disorders treated or prevented by the methods described herein include, but are not limited to, cardiovascular diseases or disorders, cardiovascular diseases and disorders associated with arteriosclerosis, such as atherosclerosis, idiopathic pulmonary fibrosis (IPF), chronic obstructive pulmonary disease (COPD), osteoarthritis, inflammatory diseases or disorders, autoimmune diseases or disorders, pulmonary diseases or disorders, neurological diseases or disorders, dermatological diseases or disorders, chemotherapeutic side effects, radiotherapy side effects, metastasis and metabolic diseases.

  本文提供了用于选择性杀死衰老细胞的衰老剂，衰老细胞与多种病理和疾病有关，包括与年龄有关的病理和疾病。如本文所述，衰老细胞相关疾病可通过施用至少一种衰老分解剂或其药物组合物来治疗或预防。本文所述方法可治疗或预防的衰老细胞相关疾病或紊乱包括但不限于心血管疾病或紊乱、与动脉硬化相关的心血管疾病和紊乱，如动脉粥样硬化、特发性肺纤维化（IPF）、慢性阻塞性肺病（COPD）、骨关节炎、炎症性疾病或紊乱、自身免疫性疾病或紊乱、肺部疾病或紊乱、神经系统疾病或紊乱、皮肤病或紊乱、化疗副作用、放疗副作用、转移和代谢性疾病。
• Secreted and transmembrane polypeptides and nucleic acids encoding the same
  申请人：Genentech, Inc.

  公开号：US20020146709A1

  公开（公告）日：2002-10-10

  The present invention is directed to novel polypeptides and to nucleic acid molecules encoding those polypeptides. Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention.

  本发明涉及新型多肽和编码这些多肽的核酸分子。本发明还提供了包含这些核酸序列的载体和宿主细胞、包含与异源多肽序列融合的本发明多肽的嵌合多肽分子、与本发明多肽结合的抗体以及生产本发明多肽的方法。
• Secreted and transmembrane polypeptides and nucleic acids enconding the same
  申请人：Genentech, Inc.

  公开号：US20030049621A1

  公开（公告）日：2003-03-13

  The present invention is directed to novel polypeptides and to nucleic acid molecules encoding those polypeptides. Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention.

  本发明涉及新型多肽和编码这些多肽的核酸分子。本发明还提供了包含这些核酸序列的载体和宿主细胞、包含与异源多肽序列融合的本发明多肽的嵌合多肽分子、与本发明多肽结合的抗体以及生产本发明多肽的方法。