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•Twelve novel 2-tethered ellipticine derivatives were synthesized in good yields.•Nine novel 2-tethered pyridocarbazole derivatives were synthesized in good yields.•Some of these compounds exhibited potent antitumor activity on HeLa S-3 cells.•Introduction of an OH group at the 9-position enhanced its antitumor activity.•Elongation of the tether had a tendency to suppress the activity of the compounds.
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