A series of novel β-carboline derivatives was synthesized and evaluated for their cytotoxic activities in vitro
against two human tumor cell lines. Most of the compounds showed moderate to potent cytotoxic activities against the
tested cell lines, in which compound 12l exhibited the most potent antiproliferative activities against KB cell line (IC50 =
4.58 µM). Preliminary mechanism research on compound 12l indicated that it could inhibit DNA intercalation and tubulin
Keywords: Antiproliferative, Antitubulin, β-Carboline Derivatives, DNA intercalation, Structure-activity relationship, Synthesis.
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