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

K. C. Nicolaou, Silvano Sanchini, David Sarlah, Gang Lu, T. Robert Wu, Daniel K. Nomura, Benjamin F. Cravatt, Beatrice Cubitt, Juan C. De La Torre, Ann Hessell, Dennis R. Burton

Research output: Contribution to journalArticle

28 Citations (Scopus)

Abstract

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 throughmodular chemical synthesis and led to the discovery of small organic molecules possessing anti-HIV and anti-arenavirus properties.

Original languageEnglish (US)
Pages (from-to)6715-6720
Number of pages6
JournalProceedings of the National Academy of Sciences of the United States of America
Volume108
Issue number17
DOIs
StatePublished - Apr 26 2011
Externally publishedYes

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Biological Products
Libraries
Arenavirus
Drug Discovery
HIV
Lead

Keywords

  • [2 + 2] photocycloaddition
  • Anti-inflammatory agents
  • Antiviral agents

ASJC Scopus subject areas

  • General

Cite this

Design, synthesis, and biological evaluation of a biyouyanagin compound library. / Nicolaou, K. C.; Sanchini, Silvano; Sarlah, David; Lu, Gang; Wu, T. Robert; Nomura, Daniel K.; Cravatt, Benjamin F.; Cubitt, Beatrice; De La Torre, Juan C.; Hessell, Ann; Burton, Dennis R.

In: Proceedings of the National Academy of Sciences of the United States of America, Vol. 108, No. 17, 26.04.2011, p. 6715-6720.

Research output: Contribution to journalArticle

Nicolaou, KC, Sanchini, S, Sarlah, D, Lu, G, Wu, TR, Nomura, DK, Cravatt, BF, Cubitt, B, De La Torre, JC, Hessell, A & Burton, DR 2011, 'Design, synthesis, and biological evaluation of a biyouyanagin compound library', Proceedings of the National Academy of Sciences of the United States of America, vol. 108, no. 17, pp. 6715-6720. https://doi.org/10.1073/pnas.1015258108
Nicolaou, K. C. ; Sanchini, Silvano ; Sarlah, David ; Lu, Gang ; Wu, T. Robert ; Nomura, Daniel K. ; Cravatt, Benjamin F. ; Cubitt, Beatrice ; De La Torre, Juan C. ; Hessell, Ann ; Burton, Dennis R. / Design, synthesis, and biological evaluation of a biyouyanagin compound library. In: Proceedings of the National Academy of Sciences of the United States of America. 2011 ; Vol. 108, No. 17. pp. 6715-6720.
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