Vidhya Thomas , D Giles 1 , Guru P M Basavarajaswamy , Amit Kumar Das , Avani Patel . Show Affiliations »
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
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 . Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
Entities: Chemical
Disease
Gene
Keywords:
Anticancer; anti-inflammatory; coumarin; docking; hydrazone; thiazole
Mesh: See more »
Substances: See more »
Year: 2017
PMID: 27592545 DOI: 10.2174/1871520616666160902094739
Source DB: PubMed Journal: Anticancer Agents Med Chem ISSN: 1871-5206 Impact factor: 2.505