𝐼𝑛 𝑆𝑖𝑙𝑖𝑐𝑜 Design, Synthesis and Evaluation of Curcumin and Its Analogues against A۵۴۹ Lung Cancer Cell Line

Curcumin and a series of its analogues synthesized via ultrasonic irradiation method, from the treatment of various substituted aromatic aldehydes with acetylacetone. The structures of these compounds are assigned by using mass spectrum, Fourier-transform infrared spectroscopy (FT-IR), electronic spectra, ۱H-NMR, and ۱۳C-NMR spectra which confirm the purpose of their structure. These series were evaluated against the A۵۴۹ lung cancer cell line. Curcumin (IC۵۰:۹۴.۲۵, SI:۳.۲۰), compound ۵ (IC۵۰:۱۰۵.۴, SI:۱.۱۷), and ۶ (IC۵۰:۱۰۴.۷, SI:۱.۲۹), were found to be the most potent anticancer agents. In comparison, curcumin is the most potent and more selective agent against A۵۴۹ lung cancer cell line. In molecular docking study of curcumin and its analogues that docked with protein active site of epidermal growth factor receptor (ID۵y۹t) using MOE calculated, the result revealed that the binding affinity of the studied compounds to EGFR affected by the substitution on the aromatic ring. Therefore, it was indicated that curcumin and compound ۲ have better binding affinity to the receptor.

کلیدواژه ها:

curcumin ، EGFR ، lung cancer A۵۴۹ ، Molecular docking ، Ultrasonic irradiation