Abstract

SYNTHESIS, ANTIOXIDANT AND CYTOTOXIC ACTIVITIES OF SOME NEW CHALCONES INCORPORATING INDOLE BASEDMELATONIN ANALOGUES

Nadia T. A. Dawoud*, S. M. Mohamed, Doaa M. M. Elbadawy, Fatma S. M. Moawed and Amel F. M. Ismail

Abstract

Melatonin (MLT) has been indicated as a possible oncostatic agent in different types of cancer, its anti-proliferative role being demonstrated in several in-vitro and in vivoexperimental models of tumors. Research on MLT related compounds has been required to optimize the maximum pharmaceutical activity with the lowest side effects. In this study a series of some new 3-(substitutedaryl)-N-(5-methoxy-1Hindol- 3-yl)ethyl) acryl amide (2a-e) has been synthesized and characterized on the basis of elemental analysis, spectral data (IR,1H-, 13C-NMR and Mass spectra). In-vitro antioxidant activity of the newly synthesized compounds was investigated by evaluating their radical scavenging activity via the DPPH assay. In addition, the cytotoxic activity of the newly synthesized compounds was evaluated against human hepatocellular carcinoma HepG2 cells. Compounds (2c, 2d,2e) exhibited a potent in-vitro cytotoxic activity than the reference drug doxorubicin, so significant implications on future clinical exploitation of these molecules in hepatocellular cancer therapeutics may be occurred.

Keywords: Melatonin, Chalcones, Antioxidant activity, Cytotoxicity, HepG2.