Identification of 3-Bromo-1-Ethyl-1H-Indole as a Potent Anticancer Agent with Promising Inhibitory Effects on GST Isozymes.

Abstract

BACKGROUND: Indole based heterocyclic compounds plays important roles in pharmaceutical chemistry due to their unexpected biological and pharmacological properties. OBJECTIVE: Herein, we describe novel biological properties (antioxidant, antimicrobial and anticancer) of 3-bromo-1-ethyl-1H-indole (BEI) structure. METHOD: BEI was synthesized from 1-Methyl-2-phenylindole and N-bromosuccinimide and were characterized by using 1H and 13C NMR. 1H and 13C NMR. Cytotoxity was determined by MTT assay. Apoptosis analysis of BEI was determined by Arthurâ„¢ imagebased Cytometer. Different methods was applied to assessed the antioxidant activity of BEI. Molecular docking studies were conducted to determine the interactions of bonding between GST isozymes and BEI. RESULTS: According to the antioxidant and antimicrobial activity assays, BEI compound showed less total antioxidant activity compared to trolox standard whereas it showed moderate antimicrobial activity against Aspergillus niger and Phytophora eryhtrospora. Notably, BEI compound demonstrated substantial selective cytotoxicity for the first time towards cancer cell lines and there existed significant decrease in the percentage of live cells treated with BEI, in comparison to the control ones. Interestingly, BEI exhibited a promising glutathione S-transferase isozymes inhibition. CONCLUSION: The results of this study suggest that BEI seems to be a promising molecule to be used in design of new anticancer agents that provide superiority to present commercial anticancer drugs.