Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Anti HIV-1 Agents 7. Discovery of 1-Hydroxy-4-chloro-9,10-anthraquinone Derivatives as New HIV-1 Inhibitors in Vitro

Author(s): Ning Huang, Qin Wang, Liu-Meng Yang, Hui Xu, Yong-Tang Zheng.

Abstract:

In continuation of our program aimed at the discovery and development of anti-HIV-1 agents, six 1-hydroxy-4- chloro-9, 10-anthraquinone derivatives (3-8) were prepared and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Compounds 4 and 6 exhibited the potent anti-HIV-1 activities with EC50 values of 9.81 and 17.90 μg/mL, and TI values of > 13.58 and > 11.17, respectively. It demonstrated that introduction of the alkylacyloxy or alkylsulfonyloxy group at the 1-position of 1-hydroxy-4-chloro-9,10-anthraquinone could afford the more promising and potent compound than that having arylacyloxy or arylsulfonyloxy one.

Keywords: 1-Hydroxy-4-chloro-9,10-anthraquinone, Acquired immunodeficiency syndrome, Human immunodeficiency virus-1, Inhibitor, 9,10-anthraquinone derivatives (AQ), reverse transcriptase (RT), nonnucleoside RT inhibitors (NNRTIs), protease inhibitors (PIs), cyanobactericidal activities, benzenesulfonyloxy group, arylacyloxy, methanesulfonyloxy group, p-chlorophenol

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Article Details

VOLUME: 8
ISSUE: 7
Year: 2011
Page: [602 - 605]
Pages: 4
DOI: 10.2174/157018011796235185
Price: $58