2'-deoxyuridine 3',5'-cyclic monophosphate | 24853-46-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 2'-deoxyuridine 3',5'-cyclic monophosphate
• 英文别名: Desoxyuridin-(3'-5')-cyclophosphat；O^3'_,O5'-hydroxyphosphoryl-2'-deoxy-uridine；1-[(4aR,6R,7aS)-2-hydroxy-2-oxo-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-6-yl]pyrimidine-2,4-dione
• CAS: 24853-46-1
• 化学式: C₉H₁₁N₂O₇P
• 分子量: 290.169
• InChiKey: MFGVUBZXOOYNCK-SHYZEUOFSA-N

物化性质

• 密度：
  1.73±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  114
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2'-deoxyuridine 5'-monophosphate N,N'-dicyclohexyl-4-morpholinecarboxamidine salt 在 N,N'-二环己基碳二亚胺 作用下， 以 吡啶 为溶剂， 反应 1.5h， 生成 2'-deoxyuridine 3',5'-cyclic monophosphate
  参考文献：
  名称：

  5-卤代和5-（三氟甲基）-2'-脱氧尿苷3'，5'-环一磷酸和中性三酯的合成及其抗肿瘤和抗病毒特性。

  摘要：

  标题二酯（11-15；卤素取代基F，Cl，Br，I）是通过DCC诱导的前体5'-单磷酸环化或2'-脱氧尿苷3'，5'-环单磷酸的直接卤化制备的。将细胞系统（L1210和Raji / 0）中11-15的抗肿瘤活性与相应核苷和5'-单磷酸酯的抗肿瘤活性进行了比较。因此，5-F-和5-CF3-2'-脱氧尿苷被证明是高活性衍生物[L1210的ID50值（微克/ mL），分别为0.002和0.06]，而5'-单磷酸酯显示出可比的效能。相应的3'，5'-环一磷酸二酯的效力降低了20-30倍，但仍具有高度的细胞抑制作用。包括11-15在内的所有衍生物对于胸苷激酶缺陷（TK-）L1210和Raji细胞的ID50值均大大提高。3'，5' -环二酯（11-15）显然不是TK细胞中核苷5'-单磷酸的有效前药来源。他们还被证明是L1210胸苷酸合成酶抑制剂的效率比5'-单磷酸酯低100-2000倍。5-取代的2'

  DOI：

  10.1021/jm00157a022

文献信息

• Mannich Base N-Oxide Drugs
  申请人：Keana John F.W.

  公开号：US20100016252A1

  公开（公告）日：2010-01-21

  Disclosed are Mannich base N-oxides of drugs containing acidic N—H groups. Pharmaceutical compositions comprising a therapeutically effective amount of Mannich base N-oxides, or a N-oxide rearrangement product, pharmaceutically acceptable salt or prodrug thereof, are also disclosed. Further, disclosed are methods of using the compounds, alone or in combination with one or more other active agents or treatments.

  本发明涉及含有酸性N-H基团的药物的Mannich碱N-氧化物。还公开了包含治疗有效量的Mannich碱N-氧化物、氧化物重排产物、药学上可接受的盐或前药的制药组合物。此外，还公开了使用该化合物的方法，单独或与一种或多种其他活性剂或治疗方法结合使用。
• ODCASE INHIBITORS AS ANTI-VIRALS AND ANTIBIOTICS
  申请人：Kotra Lakshmi P.

  公开号：US20100087388A1

  公开（公告）日：2010-04-08

  The present invention includes the utility of anti-viral and/or antibacterial effective amounts of 6-substituted nucleoside derivatives of formula (I) (e.g. 6-iodouridine and 6-iodouridine monophosphate) in the treatment or prevention of viral infections (e.g. Flavivridae, Bunyaviridae, or Togaviridae, or viral infections of hepatitis C, hepatitis B, herpes, influenza, HIV, polio, Coxsackie A/B, rhino, small pox, Ebola, West Nile, or corona virus) and/or bacterial infections (e.g. H. pylori, S. Aureus, B. anthracis, Mycobacterial tuberculosis, M. leprae, M. avium, P. aueruginosa, Streptococcal species, and Pneumocystis carinii ).

  本发明涉及式（I）的6-取代核苷衍生物（例如6-碘尿嘧啶和6-碘尿苷酸单磷酸盐）的抗病毒和/或抗细菌有效量的实用性，用于治疗或预防病毒感染（例如黄病毒科、布尼亚病毒科、托加病毒科或丙型肝炎、乙型肝炎、疱疹、流感、艾滋病毒、脊髓灰质炎、柯萨奇A/B病毒、鼻病毒、天花、埃博拉、西尼罗河或冠状病毒）和/或细菌感染（例如幽门螺杆菌、金黄色葡萄球菌、炭疽杆菌、结核分枝杆菌、麻风分枝杆菌、非结核分枝杆菌、铜绿假单胞菌、链球菌属和肺孢子菌）。
• Systems and methods for treating human inflammatory and proliferative diseases and wounds, with UCP and/or FAS antibody or other inhibitor, optionally with a fatty acid metabolism inhibitor and/or a glucose metabolism inhibitor
  申请人：Newell Evan

  公开号：US20060140953A1

  公开（公告）日：2006-06-29

  Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a UCP and/or Fas antibody or other inhibitor, or combination thereof, and a therapeutically acceptable amount of a fatty acid metabolism inhibitor and/or a therapeutically acceptable amount of a glucose metabolism inhibitor, optionally in combination with one or more chemotherpeutic agents. In preferred embodiments, the invention combines an antibody against UCP and/or Fas antigen with an oxirane carboxylic acid, represented by etomoxir, and/or with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.

  治疗炎症和增生性疾病以及伤口的系统和方法，使用 UCP 和/或 Fas 抗体或其他抑制剂，或其组合，以及治疗上可接受量的脂肪酸代谢抑制剂和/或治疗上可接受量的葡萄糖代谢抑制剂，作为药方，可选择与一种或多种化疗药物结合使用。在优选的实施方案中，本发明将抗 UCP 和/或 Fas 抗原的抗体与以依托莫西为代表的环氧乙烷羧酸和/或与以 2-脱氧-D-葡萄糖为代表的 2-脱氧葡萄糖化合物相结合。本发明的系统和方法可用于治疗耐药性或多重耐药性癌症。
• Methods and products for manipulating uncoupling protein expression
  申请人：Newell K. Martha

  公开号：US20060247199A1

  公开（公告）日：2006-11-02

  The invention is based in part on the discovery that uncoupling proteins (UCPs) are expressed in the plasma membrane of rapidly dividing cells but not of growth arrested, chemotherapy resistant cells. It has also been found according to the invention that UCP is expressed in the lysosomal membrane under certain metabolic conditions. Thus the invention is methods, products, screening assays and kits relating to the manipulation of UCP expression within cellular and intracellular membranes.

  本发明部分基于以下发现：解偶联蛋白（UCPs）在快速分裂细胞的质膜上表达，而在生长受阻的化疗耐药细胞的质膜上不表达。根据本发明还发现，在某些代谢条件下，UCP 在溶酶体膜中表达。因此，本发明是有关操纵 UCP 在细胞膜和细胞内膜上表达的方法、产品、筛选检测方法和试剂盒。
• METHODS AND PRODUCTS FOR MANIPULATING UNCOUPLING PROTEIN EXPRESSION
  申请人：UNIVERSITY OF VERMONT AND STATE AGRICULTURAL COLLEGE

  公开号：EP1194168A2

  公开（公告）日：2002-04-10