Antiviral chemistry & chemotherapy · 2015
Identification of a dibenzocyclooctadiene lignan as a HIV-1 non-nucleoside reverse transcriptase inhibitor.
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Han Ying-Shan, Xiao Wei-Lie, Xu Hongtao, Kramer Victor G, Quan Yudong, Mesplède Thibault, Oliveira Maureen, Colby-Germinario Susan P, Sun Han-Dong, Wainberg Mark A
Аннотация
BACKGROUND: Due to resistance to all classes of anti-HIV drugs and drug toxicity, there is a need for the discovery and development of new anti-HIV drugs.
METHODS: HIV-1 inhibitors were identified and biologically characterized for mechanism of action.
RESULTS: We identified a dibenzocyclooctadiene lignan, termed HDS2 that possessed anti-HIV activity against a wide variety of viral strains with EC50 values in the 1-3 µM range. HDS2 was shown to act as an NNRTI by qPCR and in vitro enzyme assays.
CONCLUSIONS: This compound provides a new scaffold for further optimization of activity through structure-guided design.
METHODS: HIV-1 inhibitors were identified and biologically characterized for mechanism of action.
RESULTS: We identified a dibenzocyclooctadiene lignan, termed HDS2 that possessed anti-HIV activity against a wide variety of viral strains with EC50 values in the 1-3 µM range. HDS2 was shown to act as an NNRTI by qPCR and in vitro enzyme assays.
CONCLUSIONS: This compound provides a new scaffold for further optimization of activity through structure-guided design.