Oligonucleotide prodrugs containing 5-fluorouracil

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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Details

4241521, C07H 2104, C07H 19073, C07K 1628

Patent

active

056633211

ABSTRACT:
Homo-oligomeric 5-fluorouridine and 5-fluorodeoxyuridine (FrU.sub.n and FdU.sub.n, n=oligomer length) are synthesized and used as a polymeric drug delivery system for production of FdUMP, the potent inhibitor of thymidylate synthase (TS) and an important target in cancer chemotherapy. Disclosed are methods of both preparing and utilizing said compositions.

REFERENCES:
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Venkataraman et al., Biochim. Biophys. Acta 741: 224-229. 1983 Month not available.
Marasco, et al., A Convenient Method for the Direct Incorporation of 5-Fluoro-2'-deoxycytidine into Oligodeoxynucleotides, J. of Org. Chem., vol. 57, 1992 Month not available.
Miwa, et al., Comparative Studies on the Antitumor and Immunosuppressive Effects of the New Fluorouracil Derivative N.sup.4 -Trimethoxybenzoyl-5'-deoxy-5-fluorocytidine and Its Parent Drug 5'-Deoxy-5-fluorouridine, Chem. Pharm. Bull., vol. 38, No. 4, pp. 998-1003, 1990 month not available.
Ouchi, et al., Synthesis and Antitumor Activity of Conjugates of 5-fluorouracil and chito-oligosaccharides Involving a Hexamethylene Spacer Group and Carbamoyl Bonds, Drug, Design and Delivery, vol. 6, pp. 281-187, 1990 month not available.
Schmidt, et al., Chemical Synthesis of 2'-deoxyoligonucleotides Containing 5-fluoro-2'-deoxycytidine, Nucleic Acids Research, vol. 20, No. 10, pp. 2421-2426, 1992 month not available.

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