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.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Molecular Modeling Based Synthesis and Evaluation of In vitro Anticancer Activity of Indolyl Chalcones
Volume: 15 Issue: 11
Author(s): Rashmi Gaur, Dharmendra K. Yadav, Shiv Kumar, Mahendra P. Darokar, Feroz Khan and Rajendra Singh Bhakuni
Affiliation:
Keywords: 1, 3-Diaryl-2-propen-1-ones, Anticancer agents, Indolyl chalcones.
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.
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Cite this article as:
Gaur Rashmi, Yadav K. Dharmendra, Kumar Shiv, Darokar P. Mahendra, Khan Feroz and Bhakuni Singh Rajendra, Molecular Modeling Based Synthesis and Evaluation of In vitro Anticancer Activity of Indolyl Chalcones, Current Topics in Medicinal Chemistry 2015; 15 (11) . https://dx.doi.org/10.2174/1568026615666150317222059
DOI https://dx.doi.org/10.2174/1568026615666150317222059 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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