Abstract

IN-VITRO AND IN-VIVO ACTIVITY OF NOVEL CHALCONES DERIVATIVES TARGETING CANCER

Abhishek Raj Joshi*, Uday Raj Sharma, Kamrudeen Samani, Gurubasvaraja Swammy, Surendra V, Manjunath PM and Prakesh T.

Abstract

We synthesized 10 different chalcone derivatives by the Claisen– Schmidt condensation methods. Here, acetonapthone was treated with various benzaldehyde derivatives to obtain the derivatives of the chalcones. The reaction takes place in an ice bath with continuous stirring for 4 to 6 hrs. The reaction medium is ethanol and uses sodium hydroxide as a catalyst to boost the reaction and the derivatives are formed as AR1 to AR10. Their characterization and identification were done by physical and chemical methods like TLC, Melting point, FTIR, NMR, and Mass spectroscopy. Out of them AR1 to AR3 are showing higher activity in case of breast cancer cell line i.e. MCF7 and MDA MB (453) whereas some shows high actions on lung cancer cell line i.e. A431 cell line. The IC50 value of the compounds AR1, AR2, and AR3 for MCF7 was found to be 24 μg, 59 μg, and 45 μg; for MDA MB (453) was found to be 50 μg, 52 μg, and 49 μg; for A431 was found to be 53 μg, 60 μg, and 46 μg respectively. In-vitro studies have been conducted on 6 different types of cell lines like MCF- 7, MDA MB (453), A431, HCT-116, HL-60, and HeLa cell lines. But the compound AR1 to AR3 is showing superior activity than standard drugs in the case of MCF-7, MDA MB (453), A431 cell lines. In the case of other cell lines, they are showing less activity than the standard drug. Their in-vivo activities were also studied by comparing their body weight, RBC count, WBC count, mean survival time, and several anti-oxidants parameters as well. All the results are expressed in p-value.

Keywords: Claisen–Schmidt condensation, cytotoxicity, Docking, EAC model, Spectroscopy, cancer cells, and anti-oxidants.