Synthesis, characterization and biological evaluation of N- substituted indolyl chalcones as anticancer, anti-inflammatory and antioxidant agents

Abstract

A series of N- substituted indolyl chalcones were synthesized and evaluated for their anticancer, anti-inflammatory and antioxidant activity. Adequate confirmation of the synthesized compounds was achieved using modern analytical techniques like FT-IR, HRMS, 1H NMR and 13C NMR spectroscopic techniques. Eighteen compounds were tested against MCF7 breast cancer cell line and monkey normal Vero cell line and calculated GI50 values from averages of 3 experiments. Compound 3a and 3 m exhibited potent activity (GI50 = <0.1 and 16.3 µM respectively) against the MCF7 (estrogen receptor-positive) cell line which was almost as good as that of standard drug adriamycin (GI50 = <0.1 µM). Synthesized compounds were also evaluated for their antioxidant and anti-inflammatory activity. Most of the N- substituted indolyl chalcones displayed excellent antioxidant and anti-inflammatory activity.