Dual Antitumor and Antifungal Potential of Terpene and Propenylbenzene Amines

Amino moieties are ubiquitous in pharmacologically active molecules. In this context, the objective of this study was to evaluate the biological activities of 24 amines derived from naturally occurring terpenes and propenylbenzenes obtained through hydroaminomethylation.

The synthesized amines were assessed for cytotoxicity against two human tumor cell lines (MDA-MB-231 and K562). Antifungal activity was also evaluated against eight clinically relevant pathogenic fungal species. Standard reference drugs (etoposide and imatinib) were included for comparison.

Several compounds exhibited cytotoxic activity, with IC50 values ranging from 25 to 60 μM, and selectivity indexes up to 7, comparable to or surpassing those of the reference drugs. Antifungal assays revealed that some terpene-derived amines were active against Cryptococcus gattii and Cryptococcus neoformans, with minimal inhibitory concentrations between 15.6 and 62.5 μM.

The results indicate that amines derived from biobased terpenes and propenylbenzenes possess promising anticancer and antifungal profiles. The cytotoxicity and selectivity observed in certain compounds, along with their activity against Cryptococcus species, highlight the potential of these amino-functionalized derivatives for future optimization.

This study demonstrates that hydroaminomethylation-derived amines from natural terpenes and propenylbenzenes show relevant cytotoxic and antifungal activities, supporting their potential as starting points for the development of new bioactive molecules.