Cytotoxic activity of (S)-goniothalamin and analogues against human cancer cells

Abstract: (R)- and (S)-Goniothalamin (1) and analogues 2–9 were efficiently prepared in high overall yield and enantiomeric purity, and their cytotoxic activities were evaluated against eight human cancer cell lines. A structure–activity relationship study (SAR) allowed us to establish the relevant structural features for the cytotoxic activity of goniothalamin analogues. In addition, we have identified non-natural form of goniothalamin (S)-1 and analogue 5 as the highest and more selective cytotoxic compounds against kidney cancer cell growth (786-0) with IC50 =4 and 5nM, respectively, and compound 8 (IC50 =4nM) as the more potent against breast cancer cells with resistance phenotype for adryamycin (NCI.ADR). [Copyright &y& Elsevier]