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.
Anti-Cancer Agents in Medicinal Chemistry
Title:Coumarin Derivatives as Anti-inflammatory and Anticancer Agents
Volume: 17 Issue: 3
Author(s): Vidhya Thomas, D. Giles, Guru P.M. Basavarajaswamy, Amit Kumar Das and Avani Patel
Affiliation:
Keywords: Anticancer, anti-inflammatory, coumarin, docking, thiazole, hydrazone.
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.Export Options
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Cite this article as:
Thomas Vidhya, Giles D., Basavarajaswamy P.M. Guru, Das Kumar Amit and Patel Avani, Coumarin Derivatives as Anti-inflammatory and Anticancer Agents, Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (3) . https://dx.doi.org/10.2174/1871520616666160902094739
DOI https://dx.doi.org/10.2174/1871520616666160902094739 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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