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A novel series of imidazo[1,2-a]pyridine based 1H-1,2,3-triazole derivatives were designed, synthesized, and evaluated for their anticancer activity against two different human cancer cell lines. Most of the synthesized compounds displayed anticancer activity with IC 50 values from 2.35 to 120.46 μM. Furthermore, compounds 9b, 9c, 9d, 9f, and 9j showed potent inhibitory activity against cancer cell lines, with IC 50 values close to that of standard drug. It is important to note that compound 9d was more potent than the standard drug cisplatin with IC 50 values of 10.89 and 2.35 μM against Hela cell line and MCF-7 cell line, respectively.

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