Cancer is a major death‐causing disease all over the world for the past few decades. A novel series of 1,2,3‐triazole tethered indole (7a‐l) derivatives have been synthesized and their structures were confirmed by 1HNMR, 13CNMR, and mass spectral data. All these compounds (7a –l) were screened for anticancer activity against two human cancer cell lines such as MCF‐7 and HepG‐2 cells by MTT assay. Compounds substituted with 4‐hydroxy, 4‐methoxy, 2‐methyl, and 3‐acetyl groups exhibited more potent activity against MCF‐7 and HepG‐2 cell lines with best IC50 values than standard reference Doxorubicin. Molecular docking studies performed on crystal structures of Aurora kinase‐1 and DNA topoisomerase‐2 alpha showed remarkable binding affinity values and key interactions as compared to the standard reference Doxorubicin.

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A series of novel 2-bromo-6-(4,5-diphenyl-1-((subtituted-phenyl-1H-1,2,3-triazol-4-yl)methyl)-1H-imidazol-2-yl)pyridine (7a-l) were synthesized and characterized by various analytical techniques. All the synthesized compounds were evaluated for their in vitro anticancer activity against two human cancer cell lines such as HT-1080 (Human fibro sarcoma cells) and Caco-2(Human colorectal adenocarcinoma cells) and IC50values were compared against standard anticancer drug doxorubicin. Among all the synthesized compounds 7b, 7c and 7f has shown potent activity against HT-1080. Similarly compounds 7b and 7c shown significant activity among all the synthesized compounds against Caco-2. Furthermore, the results were supported by molecular docking studies.