Xanthone Conjugated Amino Acids as Potential Anticancer and DNA Binding Agents: Molecular Docking, Cytotoxicity and SAR Studies

Author(s): Kadallipura P. Rakesh, Nanjudappa Darshini, Honnayakanakalli M. Manukumar, Hamse K. Vivek, Mohammed Y.H. Eissa, Doddakunche S. Prasanna*, Ningegowda Mallesha*

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 18 , Issue 15 , 2018

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Graphical Abstract:


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 respectively.

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.

Keywords: Xanthone, amino acids, anticancer, SAR, docking, doxorubicin, binding interactions, structure-activity relationship.

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Article Details

Year: 2018
Page: [2169 - 2177]
Pages: 9
DOI: 10.2174/1871520618666180903105256
Price: $65

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