biostudies-literatureUnknown29(5)Lizzadro LSaxony-AnhaltThe 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.Molecules (Basel, Switzerland)1123https://www.ebi.ac.uk/biostudies/studies/S-EPMC10934378biostudies-literatureSynthesis of a Non-Symmetrical Disorazole C₁-Analogue and Its Biological Activity.PMC10934378Schinzer DStadler MSpieß OLizzadro LReinecke SfalseSynthesis of a Non-Symmetrical Disorazole C₁-Analogue and Its Biological Activity.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.2024-01-01T00:00:00Z2024 Mar2025-04-04T21:31:09.271Z2025-04-04T21:31:09.271ZS-EPMC109343783847463510.3390/molecules29051123