A series of eight amino derivatives (3a-h) from perezone 1 were prepared by nucleophilic addition of bioactive amines v.gr. melatonin, acetyl tryptamine, tryptophan and other amino acids esters (valine, leucine and methionine). Their structures were elucidated by spectroscopy data. The cytotoxic evaluation against four human tumor cell lines PC-3, K-562, HCT-15 and SKLU-1 was performed as well as the TBARS assay for antioxidant activity. The results suggest that 1 and its isomer 4 were highly active against all cell lines, 4 was twice as potent than 1 against PC-3 and HCT-15. The derivative 3a (IC(50)=7.5 ± 0.3 μM) was more active than 1 against HCT-15 whereas 3h was selective against K-562 with IC(50)=4.5 ± 0.4 μM. The TBARS assay has shown that 3c with IC(50)=5.564 ± 0.24 μM is a potent antioxidant with superior effect comparing to α-tocopherol and moreover was more active than the precursor molecule 1.