Background: The spirocyclic compounds have always aroused a great interest
because this motif is present as structural core in a number of natural products and bioactive
compounds. In particular, the spirolactone moiety has been recognized in a wide array
of natural and non-natural scaffolds showing a variety of useful pharmacological
Methods: Extensive literature search using SciFinder (Databases: CA Plus, CAS Registry,
CAS React, Chemlist, Chemcat and Medline) and Web of Science (Database: Web of
Science Core Collection) was conducted.
Results: Nowadays, many efforts are being devoted to the discovery of new natural products
containing the promising spirolactone framework and to the disclosure of the potential
bioactivities of these chemical entities. Moreover, the medicinal relevance of many
spirolactones makes these scaffolds attractive targets for the design and development of
innovative and efficient synthetic strategies, enabling the construction of complex and
variably substituted products.
Conclusion: This review gives an overview on the recent advances in the spirolactones
field, in terms of new compounds isolated from natural sources, recently determined bioactivity
profiles and innovative synthetic approaches. The collected data demonstrate the
key role played by spirolactones in medicinal chemistry and the great attention still devoted
by the scientific community to these compounds.