Cytotoxic activity of (S)-goniothalamin and analogues against human cancer cells |
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Authors: | Fátima Angelo de Kohn Luciana K Carvalho João Ernesto de Pilli Ronaldo A |
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Affiliation: | 1. College of Chemistry and Material Sciences, South Central University for Nationalities, 182 Minyuan Road, Wuhan 430074, PR China;2. College of Pharmacy, South Central University for Nationalities, 182 Minyuan Road, Wuhan 430074, PR China |
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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 5 nM, respectively, and compound 8 (IC50 = 4 nM) as the more potent against breast cancer cells with resistance phenotype for adryamycin (NCI.ADR). |
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