Inhibitory Effects of Triterpene–Azidothymidine Conjugates on Proliferation of Human Immunodeficiency Virus Type 1 and Its Protease

Chao-mei Ma; Norio Nakamura; Masao Hattori; Takuya Kawahata; Toru Otake

doi:10.1248/cpb.50.877

Notes

Inhibitory Effects of Triterpene–Azidothymidine Conjugates on Proliferation of Human Immunodeficiency Virus Type 1 and Its Protease

Chao-mei Ma, Norio Nakamura, Masao Hattori, Takuya Kawahata, Toru Otake

著者情報

キーワード: FK 3000, azidothymidine (AZT), protease inhibition, reverse transcriptase inhibition, triterpene–AZT conjugate, human immunodeficiency virus

ジャーナルフリー

2002 年 50 巻 6 号 p. 877-880

DOI https://doi.org/10.1248/cpb.50.877

詳細

抄録

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, though AZT itself showed no PR inhibitory activity at all. However, the triterpene-FK 3000 conjugates showed neither PR inhibitory activity nor anti-HIV activity.

責任著者(Corresponding author)

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