An Expeditious Route to Fluorinated Rapamycin Analogues by Utilising Mutasynthesis

Goss, Rebecca J. M., Lanceron, Simon, Roy, Abhijeet Deb, Sprague, Simon, Nur-E-Alam, Mohammed, Hughes, David L., Wilkinson, Barrie and Moss, Steven J. (2010) An Expeditious Route to Fluorinated Rapamycin Analogues by Utilising Mutasynthesis. ChemBioChem, 11 (5). pp. 698-702. ISSN 1439-4227

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Abstract

Rapamycin is a drug with several important clinical uses. Its complex structure means that total synthesis of this natural product and its analogues is demanding and lengthy. A more expeditious approach is to utilise biosynthesis to enable the generation of otherwise synthetically intractable analogues. In order to achieve this, rules governing biosynthetic precursor substrate preference must be established. Through determining these rules and synthesising and administering suitable substrate precursors, we demonstrate the first generation of fluorinated rapamycin analogues. Here we report the generation of six new fluororapamycins.

Item Type: Article
Uncontrolled Keywords: precursor-directed biosynthesis,immunosuppressants,fluorine,derivatives,antibiotics,products,natural,biosynthesis,antitumor agents
Faculty \ School: Faculty of Science > School of Chemistry
Faculty of Science > School of Chemical Sciences and Pharmacy
Depositing User: Rachel Smith
Date Deposited: 16 Jun 2011 09:44
Last Modified: 17 Mar 2020 15:19
URI: https://ueaeprints.uea.ac.uk/id/eprint/32661
DOI: 10.1002/cbic.200900723

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