Synthesis of Methoxy-substituted Chalcones and in vitro Evaluation of their Anticancer Potential

被引：26

作者：

Ethiraj, Kannatt Radhakrishnan ^{[1
,2
]}

Aranjani, Jesil Mathew ^{[3
]}

Khan, Fazlur-Rahman Nawaz ^{[2
]}

机构：

[1] VIT Univ, Sch Adv Sci, Pharmaceut Chem Div, Vellore 632014, Tamil Nadu, India

[2] VIT Univ, Sch Adv Sci, Organ & Med Chem Res Lab, Vellore 632014, Tamil Nadu, India

[3] Manipal Univ, Manipal Coll Pharmaceut Sci, Dept Pharmaceut Biotechnol, Udupi 576104, Karnataka, India

来源：

CHEMICAL BIOLOGY & DRUG DESIGN | 2013年 / 82卷 / 06期

关键词：

apoptosis; chalcones; chromatin condensation; cytotoxicity; DNA damage; flow cytometry; DOXORUBICIN-INDUCED APOPTOSIS; DESIGN; ASSOCIATION; SYSTEM; CANCER; CELLS;

D O I：

10.1111/cbdd.12184

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 0.019m against HeLa, 0.020m against HCT15 and 0.022m against A549. Compound 3e, (3-(3,5-dimethoxyphenyl)-1-(2-naphthyl) prop-2-en-1-one) showed better IC50 values against all the three cell lines employed for the study.

引用

页码：732 / 742

页数：11

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