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