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Spiro[3.3]heptane as a Saturated Benzene Bioisostere**

Title: Spiro[3.3]heptane as a Saturated Benzene Bioisostere**
Authors: Prysiazhniuk, Kateryna; Datsenko, Oleksandr P.; Polishchuk, Oleksandr; Shulha, Stanislav; Shablykin, Oleh; Nikandrova, Yelyzaveta; Horbatok, Kateryna; Bodenchuk, Iryna; Borysko, Petro; Shepilov, Dmytro; Pishel, Iryna; Kubyshkin, Vladimir; Mykhailiuk, Pavel K.
Contributors: H2020 European Research Council
Source: Angewandte Chemie International Edition ; volume 63, issue 9 ; ISSN 1433-7851 1521-3773
Publisher Information: Wiley
Publication Year: 2024
Collection: Wiley Online Library (Open Access Articles via Crossref)
Description: 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.
Document Type: article in journal/newspaper
Language: English
DOI: 10.1002/anie.202316557
Availability: https://doi.org/10.1002/anie.202316557; https://onlinelibrary.wiley.com/doi/pdf/10.1002/anie.202316557
Rights: http://creativecommons.org/licenses/by/4.0/
Accession Number: edsbas.523E41EF
Database: BASE