Coumarin Derivatives as Anti-inflammatory and Anticancer Agents

Author(s): Vidhya Thomas, D. Giles, Guru P.M. Basavarajaswamy, Amit Kumar Das, Avani Patel

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 17 , Issue 3 , 2017

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Graphical Abstract:


Background: Inflammation substantially contributes to the development and progression of malignancies. cancer-related inflammation, has been proposed to promote tumor progression and serve as the seventh hallmark of tumor. Tumor microenvironment, products of inflammatory cells influence almost every aspect of tumorigenesis and tumor progression.

Objective: The aim of this study was to design and evaluate drug candidates targeting cancer-related inflammation.

Method: A series of 4-hydroxy- 3-(2- (2-[2- [(substituted phenyl)methylidene]hydrazin-1- yl]-1,3- thiazol-5- yl)-1- phenylethyl)-2H-chromen- 2-one (4a-j) were synthesized for its potential activity towards COX-2 inhibition and anticancer activity against MCF-7 and EAC cell lines. The structures of the synthesized compounds were elucidated using spectral data. Docking study was also performed to determine the probable binding mode of the compounds into the active site.

Results: Compound 4b showed significant anti-inflammatory and anticancer activity.

Conclusion: According to the results, it was concluded that designing compounds targeting cancer-related inflammation could be helpful in developing promising drug candidates for the treatment of cancer.

Keywords: Anticancer, anti-inflammatory, coumarin, docking, thiazole, hydrazone.

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Article Details

Year: 2017
Published on: 19 February, 2017
Page: [415 - 423]
Pages: 9
DOI: 10.2174/1871520616666160902094739
Price: $65

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