Background: Plants produce several bioactive secondary metabolites whose are used as
therapeutic agents to treat several diseases, among whom cancer. Triterpenes are secondary metabolites
that exert inhibitory activity against multiple intracellular and extracellular targets in euchariotic cells.
These targets are proteins involved in apoptosis, cell development and differentiation, angiogenesis,
metastasis and inflammatory processes. The inhibition of their functions leads to decreased cellular
growth, differentiation and migration, resulting in antitumor activity, as shown by several authors. Furthermore,
during recent years synthetic triterpenoid derivatives have also been developed to implement
potency and efficacy of starting compounds, allowing the obtainment of new agents having promising
Objective: In this review we report the latest results regarding anticancer activity of some of the most
studied triterpenes in the field, as well as of their semi-synthetic derivatives, with the aim to summarize
the role of triterpenes as molecular leads for the development of new classes of antitumor agents.
Methods: We focused on the most recent literature regarding triterpenes in cancer treatment, highlighting
the potential of developing new drugs starting from these natural compounds.
Conclusion: Several “old” triterpenes as ursolic, betulinic and oleanolic acids were recently reconsidered
as model compounds for the development of innovative anticancer agents. Their activity
against proteins involved in tumor development enhances the opportunity to exploit these compounds
as new multi-target therapeutic agents. Furthermore, the possibility to synthetize new compounds from
their natural-occurring structures could be an alternative to overcome cellular resistance to drugs and
could improve their therapeutic efficacy.