- Automated modular synthesis of Aptamer-drug conjugates for targeted drug delivery
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Aptamer-drug conjugates (ApDCs) are promising targeted drug delivery systems for reducing toxicity while increasing the efficacy of chemotherapy. However, current ApDC technologies suffer from problems caused by the complicated preparation and low control
- Wang, Ruowen,Zhu, Guizhi,Mei, Lei,Xie, Yan,Ma, Haibin,Ye, Mao,Qing, Feng-Ling,Tan, Weihong
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supporting information
p. 2731 - 2734
(2014/03/21)
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- Synthesis of cyclopentanyl carbocyclic 5-fluorocytosine ((-)-5-fluorocarbodine) using a facially selective hydrogenation approach
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An efficient synthetic route to biologically relevant (-)-5-fluorocarbodine 6 was developed. Direct coupling of N6-protected 5-fluorouracil 15 with cyclopentenyl intermediate 13, followed by formation of a macrocycle between the base and the ca
- Cho, Jong Hyun,Amblard, Franck,Coats, Steven J.,Schinazi, Raymond F.
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p. 723 - 727
(2013/03/13)
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- Novel antiviral C5-substituted pyrimidine acyclic nucleoside phosphonates selected as human thymidylate kinase substrates
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Acyclic nucleoside phosphonates (ANPs) are at the cornerstone of DNA virus and retrovirus therapies. They reach their target, the viral DNA polymerase, after two phosphorylation steps catalyzed by cellular kinases. New pyrimidine ANPs have been synthesize
- Topalis, Dimitri,Pradère, Ugo,Roy, Vincent,Caillat, Christophe,Azzouzi, Ahmed,Broggi, Julie,Snoeck, Robert,Andrei, Graciela,Lin, Jay,Eriksson, Staffan,Alexandre, Julie A. C.,El-Amri, Chahrazade,Deville-Bonne, Dominique,Meyer, Philippe,Balzarini, Jan,Agrofoglio, Luigi A.
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scheme or table
p. 222 - 232
(2011/03/22)
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- Heterocyclic nucleoside analogues: Design and synthesis of antiviral, modified nucleosides containing isoxazole heterocycles
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We have designed and synthesized novel antiviral nucleoside analogues, which consist of isoxazole rings as modified sugars and nucleobases (thymine, uracil, and 5-fluorouracil) with a methylene linker between them. These compounds represent a new class of
- Lee, Yoon-Suk,Byeang, Hyean Kim
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p. 1395 - 1397
(2007/10/03)
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- Synthesis of 1- and 3-Arylcarbonyl Derivatives of 5-Fluorouracil
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4'-Substituted 1-arylcarbonyl-5-fluorouracil derivatives were synthesized from the reaction of the potassium salt of 5-fluorouracil with one equivalent of aryl acid chloride in acetonitrile. 4'-Substituted 3-arylcarbonyl-5-fluorouracil derivatives were sy
- Perrin, John H.,Underberg, William J.,Sloan, Kenneth B.
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p. 397 - 402
(2007/10/03)
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- Synthesis of difluorocyclopropyl carbocyclic homo-nucleosides
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Racemic difluorinated carbocyclic homo-nucleoside analogues are easily accessible from (Z)-4-(benzyloxy)-2-butenyl acetate by difluorocyclopropanation using sodium chlorodifluoro acetate in diglyme at 190°C followed by Mitsunobu reactions.
- Csuk, Rene,Eversmann, Leo
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p. 6445 - 6456
(2007/10/03)
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- Nucleoside Analogues. Part 10. Synthesis of Three Unusual 5-Fluorouracil Seco-nucleosides Incorporating N-(2-Chloroethyl)-N-nitrosourea Residues
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Seco-nucleosides in which 5-fluorouracil (5-FU) is attached at N3 cannot be synthesised when the heteroatom is O by the methods effective when it is S.An N-phthaloyl representative of this class has now been made from a suitably protected pyrim
- Lucey, Neil M.,McCormick, Joan E.,McElhinney, R. Stanley
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p. 795 - 802
(2007/10/02)
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- Studies on the Synthesis of Chemotherapeutics. 10. Synthesis and Antitumor Activity of N-Acyl- and N-(Alkoxycarbonyl)-5-fluorouracil Derivatives
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A number of N-acyl and N-(alkoxycarbonyl)-5-fluorouracil derivatives possessing for example, benzoyl, o-toluyl, acetyl, propionyl, heptanoyl, etoxycarbonyl, phenoxycarbonyl, and benzyloxycarbonyl groups as N1 and/or N3 substituents w
- Kametani, Tetsuji,Kigasawa, Kazuo,Hiiragi, Mineharu,Wakisaka, Kikuo,Haga, Seiji,et al.
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p. 1324 - 1329
(2007/10/02)
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- 5-Fluorouracil derivatives
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A compound represented by the formulae: STR1 wherein R1 and R2 are as defined hereinafter, useful as an anti-cancer or anti-tumor agent.
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