Enantioselective Synthesis of Pactamycin, a Complex Antitumor Antibiotic

  • Justin T. Malinowski
    Department of Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • Robert J. Sharpe
    Department of Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
  • Jeffrey S. Johnson
    Department of Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.

抄録

<jats:title>Preparing Pactamycin</jats:title> <jats:p> Microbially derived organic compounds often have remarkably intricate structures that confer striking bioactivity, but such complexity may become an impediment to drug development. Pactamycin is one such case—a potent antibiotic used to probe ribosome structure and function that in its native form is too cytotoxic for therapeutic application. <jats:bold> Malinowski <jats:italic>et al.</jats:italic> </jats:bold> (p. <jats:related-article xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" issue="6129" page="180" related-article-type="in-this-issue" vol="340" xlink:href="10.1126/science.1234756">180</jats:related-article> ; see the Perspective by <jats:bold> <jats:related-article xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" issue="6129" page="152" related-article-type="in-this-issue" vol="340" xlink:href="10.1126/science.1236882">Codelli and Reisman</jats:related-article> </jats:bold> ) present a 15-step laboratory-scale synthesis of this molecule that offers prospects for the generation of structural analogs that could facilitate further exploratory medicinal research. </jats:p>

収録刊行物

  • Science

    Science 340 (6129), 180-182, 2013-04-12

    American Association for the Advancement of Science (AAAS)

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