Design, Synthesis, and Docking Studies of 4H-Chromene and Chromene Based Azo Chromophores: A Novel Series of Potent Antimicrobial and Anticancer Agents

Author(s): Tarek H . Afifi*, Rawda M. Okasha, Heba Alsherif, Hany E.A. Ahmed, Alaa S. Abd-El-Aziz

Journal Name: Current Organic Synthesis

Volume 14 , Issue 7 , 2017

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Graphical Abstract:


Aim and Objective: Chromenes are one of the most demanded compounds that are recognized for their unique pharmacological and biological activities. This report illustrates the synthesis of new chromene series and chromene based azo chromophores as first example and examines their biological applications in order to explore their possible biological and cytotoxic activities.

Material and Method: Using multicomponent methodology, two new families of 4H-chromene and chromene azo chromophores have been successfully synthesized. These compounds were evaluated for their antimicrobial activity as well as their cytotoxicity against three cancer cell lines. The docking simulations were performed for their structure-activity relationship analyses.

Results: Novel chromene and chromene azo chromophores have been synthesized successfully using multicomponent methodology. Several of these compounds showed significant potent antimicrobial activities compared to reference drugs. In addition, antiproliferative analysis against three target cell lines was examined. Compounds 4a, 4b, 4c, and 7c possessed significant antiproliferative activity with an IC50 of 0.3 to 2 µg/mL, while their docking study proved that the pharmacophore features played a crucial role in reducing the regulation of cancer cell signaling or apoptotic activation.

Conclusion: New derivatives of benzo chromene were obtained via multicomponent methodology. The new compounds were examined for their antimicrobial and antiproliferative activities. Molecular docking study was carried out to clarify the structural desires and target binding properties as a trial for explaining the structureactivity relationship profile

Keywords: 4H- chromenes, chromene based azo chromophores, antitumor activity, biological applications, docking simulations.

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Article Details

Year: 2017
Page: [1036 - 1051]
Pages: 16
DOI: 10.2174/1570179414666170519150520
Price: $65

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