- FLOXURIDINE SYNTHESIS
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The present invention relates to a process for the preparation of floxuridine, said process comprising reacting a compound of Formula la with a compound of Formula lla in the presence of an acid Al to provide a compound of Formula Ilia in substantially diastereomerically pure form. Floxuridine may be useful as an anti-cancer drug. Floxuridine may also be useful in the preparation of other anti-cancer drugs, e.g. NUC-3373.
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Page/Page column 38-39
(2019/04/11)
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- A hydrophilic medicament phospholipid compound, its pharmaceutical composition and application
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The invention discloses a phospholipid compound of hydrophilic drugs as well as a pharmaceutical composition and application of the phospholipid compound. The pharmaceutical composition of the phospholipid compound of the hydrophilic drugs or a combined pharmaceutical composition of the phospholipid compound of the hydrophilic drugs and a pharmacologically acceptable carrier; and the pharmaceutical composition is in the form of a liquid preparation, a solid preparation, a semisolid preparation, a capsule, granules, a gel or an injection. The pharmaceutical composition is in the form of liposome nanoparticles prepared from the phospholipid compound of the hydrophilic drugs or the phospholipid compound of the hydrophilic drugs and adjuvants, and the pharmaceutical composition is 10-1000nm in grain size. The phospholipid compound of the hydrophilic drugs and the liposome nanoparticles thereof can serve as a liquid preparation, a solid preparation, a semisolid preparation, a sterilized preparation and a sterile preparation; and the phospholipid compound of the hydrophilic drugs and the liposome nanoparticles thereof are low in toxicity, and are applicable to the efficient treatment of various tumors and the like.
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Paragraph 0197
(2018/11/22)
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- Synthesis and anticancer activity of some 5-fluoro-2′-deoxyuridine phosphoramidates
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Two series of novel 4-chlorophenyl N-alkyl phosphoramidates of 3′-O-(t-butoxycarbonyl)-5-fluoro-2′-deoxyuridine (3′-BOC-FdU) (9a-9j) and 5-fluoro-2′-deoxyuridine (FdU) (10a-10j) were synthesized by means of phosphorylation of 3′-BOC-FdU (4) with 4-chlorop
- Lewandowska, Marta,Ruszkowski, Piotr,Chojnacka, Kinga,Kleczewska, Natalia,Hoffmann, Marcin,Kacprzak, Karol,Celewicz, Lech
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p. 2330 - 2341
(2016/04/26)
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- 3'- O - And 5'- O -Propargyl Derivatives of 5-Fluoro-2'-Deoxyuridine: Synthesis, Cytotoxic Evaluation and Conformational Analysis
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A series of new 3'-O- and 5'-O-propargyl derivatives of 5-fluoro-2'-deoxyuridine (1-4) was synthesized by means of propargyl reaction of properly blocked nucleosides (2,4), followed by the deprotection reaction with ammonium fluoride. The synthesized propargylated 5-fluoro-2'-deoxyuridine analogues (1-4) were evaluated for their cytotoxic activity in three human cancer cell lines: cervical (HeLa), oral (KB) and breast (MCF-7), using the sulforhodamine B (SRB) assay. The highest activity and the best SI coefficient in all of the investigated cancer cells were displayed by 3'-O-propargyl-5-fluoro-2'-deoxyuridine (1), and its activity was higher than that of the parent nucleoside. The other new compounds exhibited moderate activity in all of the used cell lines.
- Baraniak, Dagmara,Baranowski, Daniel,Ruszkowski, Piotr,Boryski, Jerzy
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p. 178 - 194
(2016/04/19)
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- Design and Synthesis of 3′- and 5′ -O-(3-Benzenesulfonylfuroxan-4-yl)-2′-deoxyuridines: Biological Evaluation as Hybrid Nitric Oxide Donor-Nucleoside Anticancer Agents
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A group of 3′-O- and 5′ -O-(3-benzenesulfonylfuroxan-4-yl)-2′-deoxyuridines possessing a variety of substituents (H, Me, I, F, CF3) at the C-5 position of the nucleoside moiety were synthesized for evaluation as hybrid anticancer agents that ha
- Moharram, Sameh,Zhou, Aihua,Wiebe, Leonard I.,Knaus, Edward E.
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p. 1840 - 1846
(2007/10/03)
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- Synthesis and biological activity of O-alkyl-3-N-aminoacyloxymethyl-5- fluoro-2'-deoxyuridine derivatives
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In an attempt to improve the effectiveness of action of 5-fluoro-2'- deoxyuridine (FUdR), various kinds of O-alkylated water-soluble analogues were synthesized. Antitumor activities against sarcoma 180 (solid) were also evaluated. Some compounds exhibited potent activities. In particular, 3'-O- p-chlorobenzyl-3-N-aminoacyloxy-methylester derivatives were effective over a very wide range of dose and gave extremely large therapeutic ratios compared with known 5-fluorouracil (5-FU) derivatives.
- Harada, Naoyuki,Hongu, Mitsuya,Kawaguchi, Takayuki,Ohohashi, Motoaki,Oda, Kouji,Hashiyama, Tomiki,Tsujihara, Kenji
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p. 1196 - 1201
(2007/10/03)
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