Curcumin is a popular, plant-derived compound that has been extensively investigated for diverse range of biological activities. Anti-cancer activity against various types of cancers and high safety profile associated with curcumin makes it very attractive. In this study, we report the synthesis and evaluation of pyrazole and click chemistry curcumin analogues for Head and Neck cancer. MTT assay against head and neck cancer cell line CAL27 revealed that the synthesized compounds are active. Pyrazole compound showed significant inhibition on pSTAT3 (Tyr 705) phosphorylation at 20 and 30 µM. As far as other compounds, they showed potent cytotoxicity against CAL27 however these compounds didn’t show any activity on pSTAT3 phosphorylation at 10-30 µM concentration. So the compounds 3 and 5 maybe acting on different signaling pathway involved in HNSCC. Molecular docking studies revealed the possible binding mode of pyrazole compound in the SH2 domain of STAT3.

Design and synthesis of curcumin analogues for cytotoxicity against head & neck cancer

253rd National Meeting (2017)

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