Heterocylcic Based Cucumin: Desin, Synthesis and Anticancer Efficay Against Hela Cells

Author:

Al-Kerm Rana1,Al-kerm Rola1,Hamed Othman1ORCID,Sawafta Ashraf1,Qneibi Mohammad1,Berisha Avni2,Dagdage Omar3,Adwan Ghaleb1

Affiliation:

1. An-Najah National University

2. University of Prishtina: Universiteti i Prishtines Hasan Prishtina

3. Sidi Mohamed Ben Abdellah University of Fes Graduate Normal School of Fes: Universite Sidi Mohamed Ben Abdellah de Fes Ecole Normale Superieure de Fes

Abstract

Abstract 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 FT-IR, 1H NMR, 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-diphenyltetrazolium 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 and a cytostatic effect of 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.

Publisher

Research Square Platform LLC

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