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Synthesis and Biological Evaluation of Novel 2-Substituted Analogues of (-)-Pentenomycin i
Zisopoulou, Stavroula A. Bousis, Spyridon Haupenthal, Jörg Herrmann, Jennifer Müller, Rolf Hirsch, Anna K.H. Komiotis, Dimitri Gallos, John K. Stathakis, Christos I.
Zisopoulou, Stavroula A.
Bousis, Spyridon
Haupenthal, Jörg
Herrmann, Jennifer
Müller, Rolf
Hirsch, Anna K.H.
Komiotis, Dimitri
Gallos, John K.
Stathakis, Christos I.
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2020-03-17
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Abstract
A library of novel 2-substituted derivatives of the antibiotic natural product pentenomycin I is presented. The new collection of analogues is divided in two main classes, 2-alkynyl- and 2-aryl- derivatives, which are accessed by the appropriate type of palladium-catalyzed cross-coupling reaction of the 2-iodo-protected pentenomycin I with suitable nucleophiles. The new derivatives were tested for their activity against certain types of bacteria and one of them, compound 8h, was found to exhibit significant inhibitory activity against several Gram-positive bacteria but also displayed cytotoxic activity against eukaryotic cell lines.
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en
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09365214
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14372096
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European Research Council