期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 10, 页码 2174-2180出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.03.059
关键词
Quinoxaline; Chalcones; Anti-tubercular; Anti-cancer; Molecular docking
资金
- Department of Science and Technology-Government of Goa, India [6-162-2013/STE-DIR/Acct/556]
We report herein, first ever synthesis of series of novel differently substituted quinoxalinyl chalcones using Claisen Schmidt condensation, its molecular docking studies, and potential to be good anti-microbial, anti-tubercular and anti-cancer agents. The antimicrobial studies were carried out against Staphylococcus aureus, Escherichia coli and Candida albicans using disc diffusion procedure. The selected chalcones were tested for anti-cancer and cytotoxicity activity against MCF-7 cancer cell line using MTT assay method. All the synthesized compounds were screened for in vitro anti-tubercular screening against MtbH37RV strains by Alamar blue dye method. These results were compared with molecular docking studies carried out on Mycobacterium tuberculosis enzyme enoyl ACP reductase using Surflex-Dock program that is interfaced with Sybyl-X 2.0. SAR analysis for antimicrobial and antitubercular activity has also been proposed. (C) 2017 Elsevier Ltd. All rights reserved.
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