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Cancer, the second leading cause of death, demands new therapies. Small molecule drugs can provide strong and targeted therapy. Herein, we report the design and synthesis of biologically active 3-(benzo[1,3]dioxol-5-yl)-N-(3-aryl-1,8-naphthyridin-2-yl)-1,8-naphthyridin-2-amine derivatives via a microwave-assisted Buchwald–Hartwig coupling strategy and their anticancer activity evaluation. The molecular structures of the synthesized compounds were confirmed by spectroscopic methods. The synthesized compounds were evaluated for their in vitro anticancer activity against three human cancer cell lines. Several compounds demonstrated promising anticancer activity. Compounds 3e and 3h exhibited the most potent anticancer activity among the series. Compound 3e showed IC50 values of 6.37 ± 0.09 μM (MCF-7), 8.29 ± 0.76 μM (A549), and 10.22 ± 0.41 μM (SiHa), while compound 3h displayed IC50 values of 9.27 ± 0.18 μM, 11.65 ± 0.54 μM, and 15.65 ± 0.26 μM against the three cancer cell lines.
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B. et al. (2026) studied this question.
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