Coumarin Derivatives as Anti-inflammatory and Anticancer Agents.
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.


METHODS
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.


CONCLUSIONS
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.
Vidhya
V
Thomas
Department of Pharmaceutical Chemistry, Acharya & B. M. Reddy College of Pharmacy, Bangalore, Karnataka, India.
D
D
Giles
Guru P M
GPM
Basavarajaswamy
Amit Kumar
AK
Das
Avani
A
Patel
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002351:Carrageenan; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051546:Cyclooxygenase 2 / Q000378:metabolism*; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D006801:Humans; D051379:Mice; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D003374:Coumarins; D052246:Cyclooxygenase 2 Inhibitors; D002351:Carrageenan; D051546:Cyclooxygenase 2
Anticancer; anti-inflammatory; coumarin; docking; hydrazone; thiazole