Spiroheptane as a Saturated Benzene Bioisostere

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 benzo...

Full description

Saved in:

Bibliographic Details
Published in:	Angewandte Chemie International Edition Vol. 63; no. 9
Main Authors:	Prysiazhniuk, Kateryna, Datsenko, Oleksandr P, Polishchuk, Oleksandr, Shulha, Stanislav, Shablykin, Oleh, Nikandrova, Yelyzaveta, Horbatok, Kateryna, Bodenchuk, Iryna, Petro Borysko, Shepilov, Dmytro, Pishel, Iryna, Kubyshkin, Vladimir, Mykhailiuk, Pavel K
Format:	Journal Article
Language:	English
Published:	Weinheim Wiley Subscription Services, Inc 01-02-2024
Edition:	International ed. in English
Subjects:	Antineoplastic drugs Benzene Heptanes
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	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.Dedicated to the people of Ukraine
ISSN:	1433-7851 1521-3773
DOI:	10.1002/anie.202316557