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Synthesis of a Non-Symmetrical Disorazole C1-Analogue and Its Biological Activity

Authors :
Luca Lizzadro
Oliver Spieß
Silke Reinecke
Marc Stadler
Dieter Schinzer
Source :
Molecules, Vol 29, Iss 5, p 1123 (2024)
Publication Year :
2024
Publisher :
MDPI AG, 2024.

Abstract

The synthesis of a novel disorazole C1 analogue is described, and its biological activity as a cytotoxic compound is reported. Based on our convergent and flexible route to the disorazole core, we wish to report a robust strategy to synthesize a non-symmetrical disorazole in which we couple one half of the molecule containing the naturally occurring oxazole heterocycle and the second half of the disorazole macrocycle containing a thiazole heterocycle. This resulted in a very unusual non-symmetrical disorazole C1 analogue containing two different heterocycles, and its biological activity was studied. This provided exciting information about SAR (structure-activity-relationship) for this highly potent class of antitumor compounds.

Details

Language :
English
ISSN :
14203049
Volume :
29
Issue :
5
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.2bc18fbb1ee4bd09024e1ead64d0a1b
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules29051123