Inhibitory effects of triterpene-azidothymidine conjugates on proliferation of human immunodeficiency virus type 1 and its protease.

@article{Ma2002InhibitoryEO,
  title={Inhibitory effects of triterpene-azidothymidine conjugates on proliferation of human immunodeficiency virus type 1 and its protease.},
  author={Chao-Mei Ma and Norio Nakamura and Masao Hattori and Takuya Kawahata and Toru Otake},
  journal={Chemical & pharmaceutical bulletin},
  year={2002},
  volume={50 6},
  pages={877-80}
}
The conjugates of some dicarboxylic acid hemiesters of triterpenes which show potent inhibition against human immunodeficiency virus type 1 protease (HIV-1 PR) with a reverse transcriptase inhibitor azidothymidine (AZT) or anti-HIV alkaloid FK 3000 were prepared, and their inhibitory activities were investigated against HIV-induced cytopathic effects (CPE) and HIV-1 PR. Most of the triterpene-AZT conjugates showed potent anti-HIV activity as well as moderate to potent PR inhibitory activity… CONTINUE READING

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1H, d, Jϭ4.1 Hz, H-9Љ), 5.85/5.91 (1H, d, Jϭ3.3 Hz, H-7Љ), 6.56/6.58 (1H, d, Jϭ7.0 Hz, H-1Љ), 6.74 (1H, d, Jϭ7.0 Hz, H-2Љ); MS (negative-API): m/z 996

1H, d, Jϭ4.1 Hz, H-9Љ), 5.85/5.91 (1H, d, Jϭ3.3 Hz, H-7Љ), 6.56/6.58 (1H, d, Jϭ7.0 Hz, H-1Љ), 6.74 (1H, d, Jϭ7.0 Hz, H-2Љ); MS (negative-API): m/z 996

6-(FK 3000)adipoylimino]olean-12-en-28-oic Acid Methyl Ester (4f): 55.7% in yield

b-O
6-(FK 3000)adipoylimino]olean-12-en-28-oic Acid Methyl Ester (4f): 55.7% in yield

Assay MT-4 cells infected with HIV-1 (LAV-1) were used for the antiviral assay as described previously

Anti-Hiv
Assay MT-4 cells infected with HIV-1 (LAV-1) were used for the antiviral assay as described previously

HIV-1 Protease Assay The same HIV-1 PR assay kit and method were used as described previously

HIV-1 Protease Assay The same HIV-1 PR assay kit and method were used as described previously

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