4.7 Article

Design, Synthesis, and Antiviral Activity Evaluation of Phenanthrene-Based Antofine Derivatives

Journal

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
Volume 60, Issue 35, Pages 8544-8551

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jf302746m

Keywords

Phenanthrene-based antofine derivatives; antiviral activity; tobacco mosaic virus; structure-activity relationship; TMV; SAR

Funding

  1. National Key Project for Basic Research [2010CB126100]
  2. National Natural Science Foundation of China [21132003, 21121002]
  3. China Postdoctoral Science Foundation [2011M500519]
  4. National Key Technology Research and Development Program [2011BAE06B02-17, 2012BAK25B03-3]
  5. Tianjin Natural Science Foundation [11JCZDJC20500]

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On the basis of our previous structure activity relationship (SAR) and antiviral mechanism studies, a series of phenanthrene-based antofine derivatives (1-12 and 18-50) were designed targeting tobacco mosaic virus (TMV) RNA and synthesized and systematically evaluated for their antiviral activity against TMV. The bioassay results showed that most of these compounds exhibited good to excellent in vivo anti-TMV activity, of which compounds 19 and 27 displayed higher activity than commercial Ribavirin, thus emerging as potential inhibitors of plant virus. The novel concise structure provides another new template for antiviral studies.

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