Two series of novel C14 heterocycle substituted epi-triptolide derivatives as potential anticancer agents were synthesized and tested for their cytotoxicity against SKOV-3 and PC-3 tumor cell lines. The introduction of C14β-aryl heterocycle aminomethyl substituent to the leading compound was found to be an effective modification method to retain the potent anticancer activity. Meanwhile, the series of epi-triptolide derivatives (21-40) with C14α-hydroxyl group, still retained the natural product's cytotoxicity. This is apparently challenges the classical structure-activity relationship of triptolide that considers the C14β-hydroxyl group to be essential for its anticancer activity.
Keywords: Anticancer; Heterocycle; PC-3; SKOV-3; Synthesis; Triptolide.
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