Developing a new effective anticancer agent becomes an urgent need to overcome of current drug-resistance. In this study, we demonstrated that curcumin with heterocyclic moiety can function as an anticancer agent in a human. A new series of curcumin-based benzodiazepines, diazepines and diazoles were prepared using a simple one pot process. The process involved a condensation reaction of curcumin with various 1,2 diamino compounds and hydrazine. The structures of the prepared heterocycles were identified by the spectroscopic methods Fourier-Transform Infrared Spectroscopy (FT-IR), 1 H NMR (Proton Nuclear Magnetic Resonance), and 13C NMR. The in vitro anticancer activities of the synthesized curcumin-based heterocycles against HeLa cancer cells were evaluated 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 IC 50 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

Title

Sys Rev Pharm

Publisher

EManuscript Technology

Publisher Country

India

Indexing

Thomson Reuters

Impact Factor

0.62

Publication Type

Both (Printed and Online)

Volume

13

Year

2022

Pages

534-542