Molecular Modeling Based Synthesis and Evaluation of In vitro Anticancer Activity of Indolyl Chalcones

Author(s): Rashmi Gaur, Dharmendra K. Yadav, Shiv Kumar, Mahendra P. Darokar, Feroz Khan, Rajendra Singh Bhakuni.

Journal Name: Current Topics in Medicinal Chemistry

Volume 15 , Issue 11 , 2015

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Graphical Abstract:


A series of twenty one chalcone derivatives having indole moiety were synthesized and were evaluated against four human cancer cell lines. Indolyl chalcones 1a, 1b, 1d, 1f-1j, 2c, 2e, 2i showed good anticancer activity. Chalcones 1b and 1d were the most active and selective anticancer agents with IC50 values <1μg/ml and 1.51μg/ml, against WRL-68 cell line, respectively. Molecular mechanism was explored through in silico docking & ADMET studies.

Keywords: 1, 3-Diaryl-2-propen-1-ones, Anticancer agents, Indolyl chalcones.

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Article Details

Year: 2015
Page: [1003 - 1012]
Pages: 10
DOI: 10.2174/1568026615666150317222059
Price: $58

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