Synthesis and Biological Evaluation of Novel 2-Substituted ­Analogues of (–)-Pentenomycin I

Author:

Zisopoulou Stavroula A.1,Bousis Spyridon234,Haupenthal Jörg2,Herrmann Jennifer5,Müller Rolf45,Hirsch Anna K. H.234,Komiotis Dimitri6,Gallos John K.1,Stathakis Christos I.1ORCID

Affiliation:

1. Department of Chemistry, Aristotle University of Thessaloniki

2. Department for Drug Design and Optimization, Helmholtz Institute for Pharmaceutical Research (HIPS) – Helmholtz Centre for Infection Research (HZI)

3. Stratingh Institute for Chemistry, University of Groningen

4. Department of Pharmacy, Saarland University

5. Department of Microbial Natural Products, Helmholtz Institute for Pharmaceutical Research (HIPS) – Helmholtz Centre for Infection Research (HZI)

6. Department of Biochemistry and Biotechnology, University of Thessaly

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.

Funder

European Research Council

Horizon 2020

Publisher

Georg Thieme Verlag KG

Subject

Organic Chemistry

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