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Synthesis and Biological Activity of Octaketides from the Cytosporone Family

: Delius, M. von; Le, C.M.; Ellinger, B.; Kuzikov, M.; Gul, S.; Dong, V.M.


Israel journal of chemistry 57 (2017), Nr.10-11, S.975-981
ISSN: 0021-2148
ISSN: 1869-5868
Fraunhofer IME ()

Cytosporone B and its simple analogues (e. g., amoitone B) were recently identified as unique agonists for nuclear orphan receptor Nur77. In this study, we have developed an aldehyde C‐H activation method for preparing natural and designer analogues from the cytosporone family. In addition, a comprehensive investigation of the compounds’ biological activities and pharmacological liabilities has been conducted and new structure activity relationships (SAR) were derived from the data. Most notably, we found that increased cytotoxicity can be obtained by virtue of fluorine substitution on the hydrophobic acyl chain.