Method of treating cancer with homo-oligonuleotides of 5-FU 5'-m

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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Other Related Categories

536 255, 536 256, A61K 3170, C07H 2104

Type

Patent

Status

active

Patent number

056145055

Description

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:
Marasco, et al., A Convenient Method for the Direct Incorporation of 5-Fluoro-2'-deoxycytidine into Oligodeoxynucleotides, J. of Org. Chem., vol. 57, 1992, pp. 6363-6365.
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.
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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