Identification of a dibenzocyclooctadiene lignan as a HIV-1 non-nucleoside reverse transcriptase inhibitor.

Q2 Pharmacology, Toxicology and Pharmaceutics
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.

Abstract Image

Abstract Image

二苯并环二烯木脂素作为HIV-1非核苷类逆转录酶抑制剂的鉴定。
背景:由于各类抗hiv药物的耐药性和药物毒性,需要发现和开发新的抗hiv药物。方法:鉴定HIV-1抑制剂并对其作用机制进行生物学表征。结果:我们鉴定了一种名为HDS2的二苯并环二烯木脂素,它对多种病毒株具有抗hiv活性,EC50值在1-3µM范围内。通过qPCR和体外酶分析显示HDS2具有NNRTI的作用。结论:该化合物通过结构导向设计为进一步优化活性提供了新的支架。
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来源期刊
Antiviral Chemistry and Chemotherapy
Antiviral Chemistry and Chemotherapy Pharmacology, Toxicology and Pharmaceutics-Pharmacology
CiteScore
5.20
自引率
0.00%
发文量
5
审稿时长
15 weeks
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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