Affiliation:
1. Enamine Ltd. Winston Churchill Str. 78 02094 Kyiv Ukraine
2. V. P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry NAS of Ukraine 02094 Kyiv Ukraine
3. Bienta Winston Churchill Str. 78 02094 Kyiv Ukraine
Abstract
AbstractThe 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.
Funder
H2020 European Research Council
Subject
General Chemistry,Catalysis