Ying-Shan Han, Wei-Lie Xiao, Hongtao Xu, Victor G Kramer, Yudong Quan, Thibault Mesplède, Maureen Oliveira, Susan P Colby-Germinario, Han-Dong Sun, Mark A Wainberg
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引用次数: 9
Abstract
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.
期刊介绍：
Antiviral Chemistry & Chemotherapy publishes the results of original research concerned with the biochemistry, mode of action, chemistry, pharmacology and virology of antiviral compounds. Manuscripts dealing with molecular biology, animal models and vaccines are welcome. The journal also publishes reviews, pointers, short communications and correspondence.
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