Background: Amino acids conjugated with heterocyclic molecules are well known for their effective
bioactive properties. In search of effective anticancer agents, a series of xanthone linked amino acids 2-23 were
synthesized and tested for in vitro anticancer activity.
Methods: In vitro anticancer activity of the synthesized xanthone linked amino acids 2-23 are tested against three
different cancer cell lines MCF-7, MDA-MB-435 and A549 by MTT assay and validated by DNA binding and
molecular docking approaches. Doxorubicin and ethidium bromide used as standard and positive control
Results: Compounds 7, 8 and 9 exhibited potent anticancer activity against tested cancer cell lines and DNA binding
study using methyl green. In the molecular docking study, binding interactions of the most active compounds 7, 8
and 9 were confirmed to molecular surface of DNA.
Conclusion: Structure-Activity Relationship (SAR) showed that the aromatic and hydrophobic amino acids
(phenylalanine, tyrosine, and tryptophan) favoured the DNA binding studies and anticancer activity whereas,
aliphatic amino acids showed least anticancer activity.