Method for preparing poly (FdU).sub.n

Details Method for preparing poly (FdU).sub.n Method for preparing poly (FdU).sub.n

1995-09-11

1998-04-21

Kunz, Gary L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 253, C07H 102, C07H 2104

Patent

active

057419000

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 thymidyalte synthase (TS) and an important target in cancer chemotherapy. Disclosed are methods of both preparing and utilizing said compositions.

REFERENCES:
Marasco, et al., A Convenient Method for the Direct Incorporation of 5-Fluoro-2'-deoxycytidine into Oligodeoxynucleotides, J. of Org. Chem., vol. 57, 1992.
Miwa, et al., Comparative Studies on the Antitumor and Immunosuppresive Effects of the New Fluorouracil Derivatives 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.
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.
Schmidt, et al., Chemical Synthesis of 2'-deoxyoligonucleotides Containing 5-fluoro-2'-deoxycytidine, Nucleic Acids Research, vol. 20, No. 10, pp. 2421-2426, 1992.

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