Synthesis of Novel Series of Cyclopropyl‐Biphenyl Functionalized Triazole Analogues and Evaluating Their Anticancer Potential

ABSTRACT Developing effective anticancer agents remains a critical preference in medicinal chemistry because of the limitations of current and traditional therapies, which include multidrug resistance and systemic toxicity. A novel series of cyclopropyl‐biphenyl tethered‐1,2,3‐triazolderivatives was synthesized via click chemistry for analyzing their cytotoxic potential. Commercially available 4'‐bromo‐[1,1'‐biphenyl]‐4‐ol procured for propargylation, Suzuki reaction, and click reaction via intermediate 4‐cyclopropyl‐4'‐(prop‐2‐yn‐1‐yloxy)‐1,1'‐biphenyl. All the synthesized derivatives were characterized based on 1 H NMR, 13 C NMR, and mass spectrometry. The prepared triazole derivatives were evaluated in vitro for their anticancer potential against cell lines A‐549 and MCF‐7. Amongst the tested compounds, 7e, 7f, and 7 g were found to exhibit substantial activity against the tested cell lines. The presence of functional groups in tested compounds 4‐nitro‐2‐chloro (7f)_IC 50 values against A‐549 is 6.06 and against MCF‐7 is 6.47), 4‐nitro (7e)_IC 50 values against A‐549 is 7.10 where as in MCF‐7 is 6.03) and 4‐nitro‐2‐methoxy (7g)_IC 50 values against A‐549 is 6.06 where as in MCF‐7 is (10.47) showed prominent activity in the tested cell lines. Based on this study, it could be inferred that the presence of an electronegative substituent (especially a 4‐nitro substituent) on the phenyl ring increases anticancer activity. Although preliminary, the results support considering these derivatives as potential leads for anticancer drug development.