In vitro bioassessment of novel δ- carboline derivatives as an antiproliferative agent

Abstract

Several carboline derivatives are anticancer agents and studied for antiproliferative action against various cancer cells. Based on the preliminary analysis using insilico strategies, we have selected eight compounds for the study. All compounds have been synthesised and characterised for their purity and chemical composition. Antiproliferative activity was assessed by insilico Carcinogenicity assay, Cytotoxicity analysis by sulphorhodamine B, Antiproliferation assay and DNA damage analysis. The cytotoxic effects of the CH5, CH17, CH29, CH34, CH37, CH39, CH42 and CH47 on Vero, HeLa, A549, BRL3A, HCT116, and MCF7 were determined using the SRB assay. CH5, CH34, CH37 and CH42 was the most potent cytotoxic towards HCT116 cells with CTC₅₀ value of 62.1 ± 0.19, 47.1 ± 0.41, 78.5 ± 1.26 and 32.1 ± 1.11 µg/ml respectively. The assay revealed a noticeable reduction in cell number for CH5 and CH37 tested except CH34 and CH42. CH5 and CH37 observed cytotoxic effects were found to destroy the cells according to time, and cell viability decreased with that time length. To learn their role in cell death, CH5 and CH37 were therefore taken up for a further screening. This study suggested that CH5 and CH37 had a separate mechanism of action to kill and that in the cell line. Such results will provide enrichment of scientific knowledge on the molecular mechanism and target therapies of CH5 and CH37, thereby potentially helpful for patients with Colon cancer.