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Aziridines are known since long time as alkylating compounds, thus dangerous products that induced a number of cancers. However, modified structures derived from amino acids allowed us obtain some novelties that showed interesting anti-cancer activity that might open new therapeutic gates. Besides inclusion of aziridines into beta-cyclodextrin might boost the synthesis of compounds that include such behaviour as solubility, and stability while maintaining their biological activity, overcoming a number of known side effects.