Compounds for the suppression of HIV Tat transactivation

Details Compounds for the suppression of HIV Tat transactivation Compounds for the suppression of HIV Tat transactivation

1996-04-04

1997-09-02

Rollins, John W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

C-o-group doai

514885, 514934, A61K 3105

Patent

active

056632096

ABSTRACT:
The present invention reveals the isolation, purification and characterization from the creosote bush Larrea tridentata of compounds of the structural formula: ##STR1## where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of HO--, CH.sub.3 O-- and CH.sub.3 (C.dbd.O)O--, provided that R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are not each HO-- simultaneously. Each compound is a derivative of 1,4-bis-(3,4-dihydroxyphenyl)-2,3-dimethylbutane (nordihydroquaiaretic acid, NDGA). In addition, NDGA and each derivative can be used in a method to suppress Tat transactivation of a lentivirus, including the HIV virus, in a cell by administering NDGA or a derivative of NDGA to the cell.

REFERENCES:
patent: 5276060 (1994-01-01), Neiss et al.
Huang et al, "Regulation of HIV Promoter Activities in Human Embryonal Carcinoma Cells", NTERA-2, Aids and Human Retroviruses--Gene Regulation and Aids, pp. 147-160.
Giza et al, Gene, 78:73-84 (1989).
Staal et al, Aids Research and Human Retroviruses, 9(4):299-306 (1993).
Gisvold et al, Lignans from Larrea divaricata, 63(12):1905-1907 (Dec., 1974).
Perry et al, J. Org. Chem., 37(26):4371-4376 (1972).

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