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Article Abstract
Scale-up isolation of (+)-(5)-(8)-(14)-mycothiazole () from Vanuatu specimens of to semisynthesize (+)-(5)-(8)-8--acetyl-(14)-mycothiazole () revealed a new diastereomer, (-)-(5)-(8)-(14)-mycothiazole (). The structure of was determined using HRMS, NMR, and comparing optical rotation to (-)-(5)-(8)-(14)-mycothiazole () and . The maximum tolerated dose of in mice was 0.1 mg/kg. The IC of in PANC-1 and HepG2 cancer cell lines was 111.6 and 115.0 nM. Evaluation of in showed similar oxygen consumption compared to -, and all compounds significantly increased the lifespan. The orientation at Δ is crucial for picomolar cytotoxicity but not for mitochondrial inhibition.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11534373 | PMC |
| http://dx.doi.org/10.1021/acs.jnatprod.4c00691 | DOI Listing |
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