Design, synthesis, and biological evaluation of a biyouyanagin compound library

Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6715-20. doi: 10.1073/pnas.1015258108. Epub 2011 Jan 18.


Modern drug discovery efforts rely, to a large extent, on lead compounds from two classes of small organic molecules; namely, natural products (i.e., secondary metabolites) and designed compounds (i.e., synthetic molecules). In this article, we demonstrate how these two domains of lead compounds can be merged through total synthesis and molecular design of analogs patterned after the targeted natural products, whose promising biological properties provide the motivation. Specifically, the present study targeted the naturally occurring biyouyanagins A and B and their analogs through modular chemical synthesis and led to the discovery of small organic molecules possessing anti-HIV and anti-arenavirus properties.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Arenaviridae Infections / drug therapy
  • Arenavirus*
  • Cell Line
  • HIV Infections / drug therapy
  • HIV*
  • Humans
  • Molecular Structure
  • Sesquiterpenes / chemical synthesis*
  • Sesquiterpenes / chemistry*
  • Sesquiterpenes / pharmacology
  • Spiro Compounds / chemical synthesis*
  • Spiro Compounds / chemistry*
  • Spiro Compounds / pharmacology


  • Anti-HIV Agents
  • Sesquiterpenes
  • Spiro Compounds
  • biyouyanagin A
  • biyouyanagin B