5-fluoro-1-((4R,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-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: 5-fluoro-1-((4R,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione
• 英文别名: 5-fluoro-1-[(4R,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione
• 化学式: C₉H₁₁FN₂O₅
• 分子量: 246.195
• InChiKey: ODKNJVUHOIMIIZ-CQMSUOBXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  99.1
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• AMPHIPHILIC DRUG-DRUG CONJUGATES FOR CANCER THERAPY, COMPOSITIONS AND METHODS OF PREPARATION AND USES THEREOF
  申请人：Shanghai Jiao Tong University

  公开号：US20150031644A1

  公开（公告）日：2015-01-29

  The invention provides novel amphiphilic drug-drug conjugates useful as cancer therapeutics, and compositions and methods thereof.

  这项发明提供了作为癌症治疗药物有用的新型两性药物-药物共轭物，以及相关的组合物和方法。
• SYSTEM AND METHODS FOR IDENTIFYING INDIVIDUALS AT RISK FOR SYSTEMIC FLUOROPYRIMIDINE TOXICITY
  申请人：Cohen James M.

  公开号：US20080241068A1

  公开（公告）日：2008-10-02

  The present disclosure is related to methods and tests for identifying individuals at risk for systemic toxicity to a substance by administering a topical dose of the substance to the individual and observing any topical response to that substance. In particular, the present disclosure provides methods and tests for determining if an individual is at risk for fluoropyrimidine, such as 5-fluorouracil, toxicity or has a dihydropyrimidine dehydrogenase deficiency by exposing the skin of the individual to a dose of a fluoropyrimidine, such as 5-fluoruracil, using a transdermal skin patch. An inflammatory response of the skin indicates the risk of the individual to such toxicity or enzyme deficiency.
• F10 Inhibits Growth of PC3 Xenografts and Enhances the Effects of Radiation Therapy
  申请人：WAKE FOREST UNIVERSITY

  公开号：US20170151240A1

  公开（公告）日：2017-06-01

  Chemotherapy remains of limited use for the treatment of prostate cancer with only one drug, docetaxel, demonstrating a modest survival advantage for treatment of late-stage disease. Data from the NCI 60 cell line screen indicated that the castration-resistant prostate cancer cell lines PC3 and DU145 were more sensitive than average to the novel polymeric fluoropyrimidine (FP), F10, despite displaying less than average sensitivity to the widely-used FP, 5FU. In an embodiment of the present invention, F10 treatment of PC3 xenografts results in a significant survival advantage (treatment to control ratio (T/C) days=18; p<0.001; n=16) relative to control mice treated with saline. F10 (40 mg/kg/dose) was administered via jugular vein catheterization 3-times per week for five weeks. This aggressive dosing regimen was completed with no drug-induced weight loss and with no evidence of toxicity. F10 was also shown to sensitize PC3 cells to radiation and F10 was also shown to be a potent radiosensitizer of PC3 xenografts in vivo with F10 in combination with radiation resulting in significantly greater regression of PC3 xenografts than radiation alone. The results indicate that F10 in this pre-clinical setting is an effective chemotherapeutic agent and possesses significant radiosensitizing properties.
• ANTI-FLAVIVIRUS COMPOUNDS AND METHODS OF USE
  申请人：FLORIDA STATE UNIVERSITY RESEARCH FOUNDATION, INC.

  公开号：US20200197369A1

  公开（公告）日：2020-06-25

  The present invention concerns the use of compounds and compositions for the treatment or prevention of Flavivirus infections, such as dengue virus infections and Zika virus infections. Aspects of the invention include methods for treating or preventing Flavivirus virus infection, such as dengue virus and Zika virus infection, by administering a compound or composition of the invention, to a subject in need thereof; methods for inhibiting Flavivirus infections, such as dengue virus and Zika virus infections, in a cell in vitro or in vivo; pharmaceutical compositions; packaged dosage formulations; and kits useful for treating or preventing Flavivirus infections, such as dengue virus and Zika virus infections.
• METHOD FOR INHIBITING ZIKA VIRUS INFECTION
  申请人：FLORIDA STATE UNIVERSITY RESEARCH FOUNDATION, INC.

  公开号：US20220323420A1

  公开（公告）日：2022-10-13

  The present invention concerns the use of compounds and compositions for the treatment or prevention of Flavivirus infections, such as dengue virus infections and Zika virus infections. Aspects of the invention include methods for treating or preventing Flavivirus virus infection, such as dengue virus and Zika virus infection, by administering a compound or composition of the invention, to a subject in need thereof; methods for inhibiting Flavivirus infections, such as dengue virus and Zika virus infections, in a cell in vitro or in vivo; pharmaceutical compositions; packaged dosage formulations; and kits useful for treating or preventing Flavivirus infections, such as dengue virus and Zika virus infections.