Phosphotriester type biologically active compounds

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

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536 2671, 536 2672, 536 2674, 536 268, 536 269, 544243, 544264, C07H 100, C07H 1900

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active

057707251

ABSTRACT:
Compounds of formula RO--P(.dbd.O)(OR)--Nu where: each R is, independently, --(CH.sub.2).sub.n --S--X; X is --C(.dbd.Z) (Y) or --S--U; Z is O or S; Y and U are alkyl, aryl or saccharide groups optionally substituted with OH, SH or NH groups; n is 1 to 4; and Nu is a nucleoside which comprises a ribose or deoxyribose sugar portion covalently bound to a base portion.

REFERENCES:
patent: 5430136 (1995-07-01), Urdea et al.
patent: 5430138 (1995-07-01), Urdea et al.
Hao, Z. et al., "Potent DNA Chain Termination Activity and Selective Inhibition of Human Immunodeficiency Virus Reverse Transcriptase by 2', 3'--Dideoxyuridine-5'-triphosphate", Molecular Pharmacology 1990, 37, 157-163.
Hao, Z. et al, "2', 3'-Dideoxyuridine Triphosphate: A Potent Inhibitor of HIV Reverse Transcriptase", Proceedings of AACR 1988, 29, 348.
Matthes, E. et al., "Inhibition of HIV-Associated Reverse Transcriptase By Sugar-Modified Derivatives of Thymidine 5'-Triphosphate in Comparison to Cellular DNA Polymerases .alpha. and .beta.", Biochemical and Biophysical Research Communications 1997, 148(1), 78-85.
Rosenberg et al., "Synthesis of Potential Prodrugs and Metabolites of 9-(S)-(3-Hydroxy-2-Phosphonylmethoxypropyl)Adenine", Collection Czechoslovak Chem. Comm. 1987, 52, 2792-2800.

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