Journal
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
Volume 108, Issue 17, Pages 6715-6720Publisher
NATL ACAD SCIENCES
DOI: 10.1073/pnas.1015258108
Keywords
[2+2] photocycloaddition; anti-inflammatory agents; antiviral agents
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Funding
- National Institutes of Health (USA)
- Skaggs Institute for Chemical Biology
- Universita degli Studi di Urbino Carlo Bo
- Japan Society for the Promotion of Science
- Natural Sciences and Engineering Research Council of Canada
- National Institute on Drug Abuse [K99DA030908]
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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.
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