Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Synthesis, Biological Evaluation and In Silico Study of β-Chloro Vinyl Chalcones as Inhibitors of the TNF-α, IL-6 With Anticancer and Antioxidant Activity

Author(s): Babasaheb P. Bandgar, Baliram S. Hote, Shivraj H Nile.


A series of novel β-chloro vinyl chalcones have been synthesized from substituted (Z) – 3 – chloro – 3- phenylacraldehydes with 1-(3 – bromo – 2 – hydroxyl-4,6- dimethoxyphenyl)ethanone by Claisen-Schmidt condensation reaction. Compounds were screened for anti-inflammatory, anticancer and antioxidant activity. Compounds 6a, 6d and 6f revealed promising anti-inflammatory activity (87 – 99 %) with less cytotoxicity (4 – 9 %) at 10 µ M. Compounds 6a, 6d, 6e and 6f having significant anticancer activity (71 – 83 %). Bioavailability of compounds were checked by in vitro cytotoxicity and confirmed to be nontoxic. Structure activity relationship and in silico drug relevant properties of compounds revealed as potential candidates for future drug discovery study.

Keywords: Anti-inflammatory activity, Anticancer activity, Antioxidant activity, In silico, luekotrienes, Claisen-Schmidt condensation reaction, Reactive oxygen species (ROS), cytotoxicity, Bioavailability, cytokines, TNF-α, atherosclerosis, rheumatoid arthritis (RA), haematopoiesis

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Article Details

Year: 2011
Page: [725 - 732]
Pages: 8
DOI: 10.2174/157018011796576051
Price: $58