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A library of bile-acid-appended triazolyl aryl ketones was synthesized and characterized by detailed spectroscopic techniques such as ¹H and ¹³C NMR, HRMS and HPLC. All the synthesized conjugates were evaluated for their cytotoxicity at 10 µM against MCF-7 (human breast adenocarcinoma) and 4T1 (mouse mammary carcinoma) cells. In vitro cytotoxicity studies on the synthesized conjugates against MCF-7 and 4T1 cells indicated one of the conjugate <b>6cf</b> to be most active against both cancer cell lines, with IC₅₀ values of 5.71 µM and 8.71 µM, respectively, as compared to the reference drug docetaxel, possessing IC₅₀ values of 9.46 µM and 13.85 µM, respectively. Interestingly, another compound <b>6af</b> (IC₅₀ = 2.61 µM) was found to possess pronounced anticancer activity as compared to the reference drug docetaxel (IC₅₀ = 9.46 µM) against MCF-7. In addition, the potent compounds (<b>6cf</b> and <b>6af</b>) were found to be non-toxic to normal human embryonic kidney cell line (HEK 293), as evident from their cell viability of greater than 86%. Compound <b>6cf</b> induces higher apoptosis in comparison to <b>6af</b> (46.09% vs. 33.89%) in MCF-7 cells, while similar apoptotic potential was observed for <b>6cf</b> and <b>6af</b> in 4T1 cells. The pharmacokinetics of <b>6cf</b> in Wistar rats showed an MRT of 8.47 h with a half-life of 5.63 h. Clearly, these results suggest <b>6cf</b> to be a potential candidate for the development of anticancer agents.