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Angew. Chem. Int. Ed. 2024, 63 (9), e202316557

DOI: 10.1002/anie.202316557

Prysiazhniuk K.; Datsenko O.; Polishchuk O.; Shulha S.; Shablykin O.; Nikandrova Y.; Horbatok K.; Bodenchuk I.; Borysko P.; Shepilov D.; Pishel I.; Kubyshkin V.; Mykhailiuk P.

The spiro[3.3]heptane core, with the non-coplanar exit vectors, was shown to be a saturated benzene bioisostere. This scaffold was incorporated into the anticancer drug sonidegib (instead of the meta-benzene), the anticancer drug vorinostat (instead of the phenyl ring), and the anesthetic drug benzocaine (instead of the para-benzene). The patent-free saturated analogs obtained showed a high potency in the corresponding biological assays.

 

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