Synthesis, Characterisation, and In Vitro Anticancer Activity of Curcumin Analogues Bearing Pyrazole/Pyrimidine Ring Targeting EGFR Tyrosine Kinase

• Published in: BioMed research international Vol. 2013; no. 2013; pp. 1 - 14
• Main Authors: Jadav, Surender Singh, Yasmin, Sabina, Khalilullah, Habibullah, Ahsan, Mohamed Jawed, Govindasamy, Jeyabalan
• Format: Journal Article
• Language: English
• Published: Cairo, Egypt Hindawi Publishing Corporation 01.01.2013; Hindawi Limited
• Subjects: Binding Sites - drug effects; Cancer; Cancer therapies; Cell Line, Tumor - drug effects; Crystallography, X-Ray; Curcumin - administration & dosage; Curcumin - analogs & derivatives; Curcumin - chemical synthesis; Cytotoxicity; Humans; Hydrogen bonds; Kinases; Ligands; Molecular Docking Simulation; Pharmaceuticals; Protein Kinase Inhibitors - administration & dosage; Protein Kinase Inhibitors - chemical synthesis; Pyrazoles - administration & dosage; Pyrazoles - chemical synthesis; Pyrimidines - administration & dosage; Pyrimidines - chemical synthesis; Receptor, Epidermal Growth Factor - antagonists & inhibitors; Receptor, Epidermal Growth Factor - chemistry; Receptor, Epidermal Growth Factor - metabolism
• ISSN: 2314-6133; 2314-6141
• DOI: 10.1155/2013/239354

In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening protocol. There were 10 tested compounds among 14 synthesized compounds, which showed potent anticancer activity in both one-dose and 5-dose assays. The most active compound of the series was 3,5-bis(4-hydroxy-3-methylstyryl)-1H-pyrazole-1-yl(phenyl)methanone (10) which showed mean growth percent of −28.71 in one-dose assay and GI50 values between 0.0079 and 1.86 µM in 5-dose assay.