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Extending the Structure‐Activity Relationship of Disorazole C1: Exchanging the Oxazole Ring by Thiazole and Influence of Chiral Centers within the Disorazole Core on Cytotoxicity

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The synthesis of novel disorazole C1 analogues is described and their biological activity as cytotoxic compounds is reported. Two regions of the molecules were examined for structural modification: 1. Replacement of the heterocyclic moiety by an exchange of the oxazole ring by a thiazole; and 2. Evaluation of the influence of the absolute configuration.


Abstract

The synthesis of novel disorazole C1 analogues is described and their biological activity as cytotoxic compounds is reported. Based on our convergent entry to the disorazole core we present a flexible and robust strategy to construct a variety of interesting new analogues. In particular, two regions of the molecules were examined for structural modification: 1. Replacement of the heterocyclic moiety by an exchange of the oxazole ring by a thiazole; and 2. Evaluation of the influence of the absolute configuration of the chiral centers of the molecule. Predicated on our flexible strategy we were able to construct all analogues in an efficient way and could perform an exciting SAR (structure-activity-relationship) study to obtain insight in the cytotoxic activity influenced by the chiral centers of the disorazole core.

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