Heterocylcic Based Curcumin: Design, Synthesis and Anticancer Efficacy against HeLa Cells
Publication Type
Original research

ABSTRACT Developing a new effective anticancer agent becomes an urgent need to overcome of current drug-resis-tance. In this study, we demonstrated that curcumin with heterocyclic moiety can function as an antican-cer agent in a human. A new series of curcumin-based benzodiazepines, diazepines and diazoles were pre-pared using a simple one pot process. The process involved a condensation reaction of curcumin with structures of the prepared heterocycles were identi-fied by the spectroscopic methods Fourier-Transform Infrared Spectroscopy (FT-IR), 1H NMR (Proton Nuclear Magnetic Resonance), and 13C NMR. The in vitro an-ticancer activities of the synthesized curcumin-based heterocycles against HeLa cancer cells were evalu-ated by the 3-[4,5-dimethylthiazole-2-yl]-2,5-diphen-yltetrazolium bromide (MTT) assay. The viability of HeLa cells was reduced in the range of 4.48%-14.57% within the studied concentrations. Curcumin-based diazepine 6 showed the highest cytotoxic effect on the HeLa cells at all concentrations. It reduced the viability of the tested HeLa cells in range of 4.48% for the 400 μg/ml concentration to 4.95% for the 12.5 μg/ml concentration. Moreover, heterocyclic 6 showed the highest cytotoxic and cytostatic effect among the tested heterocyclics against HeLa cells. It exhibited IC50 (Half-maximal inhibitory concentration) and a cytostatic effect of 0.4572 and 0.08515 μg/ ml, respectively at a nontoxic level, as the control L6 cells showed cytotoxic and cytostatic effect with IC50 values of 22.47 and 1.977 μg/ml, respectively. This study revealed that, the prepared curcumin-based compounds exhibit a promising anticancer activity against HeLa cancer cells at a nontoxic concentration. Keywords: Curcumin, Benzodiazepine, Diazole, 3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT), Anticancer, HeLa cells *Correspondence: Othman Hamed, Department of Chemistry, An-Najah National University, Nablus, Pal-estinian Territories, E-mail: ohamed@najah

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Medknow Publications
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