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Synthesis of Methoxy‐substituted Chalcones and in vitro Evaluation of their Anticancer Potential
Author(s) -
Ethiraj Kannatt Radhakrishnan,
Aranjani Jesil Mathew,
Khan FazlurRahman Nawaz
Publication year - 2013
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12184
Subject(s) - hela , cytotoxicity , chemistry , in vitro , comet assay , apoptosis , cytotoxic t cell , stereochemistry , cell culture , a549 cell , dna , microbiology and biotechnology , dna damage , biochemistry , biology , genetics
Methoxy‐substituted chalcones, 3 were obtained using simple, efficient method from 2‐naphtylethanone, 1 and aromatic aldehydes, 2. The in vitro cytotoxicity activities of the chalcones against a panel of three human cancer cell lines were explored. The tested compounds were found to possess significant cytotoxic activity. The DNA strand break and damage was quantified through alkaline comet assay, flow cytometric analysis, and chromatin condensation studies, which revealed the apoptotic nature of the compounds. Compound 3c, (3‐(3,4,5‐trimethoxyphenyl)‐1‐(2‐naphthyl) prop‐2‐en‐1‐one) showed highest cytotoxicity of 0.019 μ m against HeLa, 0.020 μ m against HCT 15 and 0.022 μ m against A549. Compound 3e, (3‐(3,5‐dimethoxyphenyl)‐1‐(2‐naphthyl) prop‐2‐en‐1‐one) showed better IC 50 values against all the three cell lines employed for the study.