Keywords
in vitro studies
anticancer agents
antitumor activity
etoposide
N-heterocyclic compounds
natural products
phaeosphaeride A
sulfides
Abstract
New C(6)-derivatives of natural phaeosphaeride A (PPA) modified with pharmacophoric nitrogen heterocyclic groups have been synthesized. The reaction of 1,2,4-triazole with PPA mesylate produced both the product of the expected substitution of the methanesulfonate group and the PPA derivative with two 1,2,4-triazole groups: at the C(6) atom and the exocyclic C=C bond. The synthesized compounds, with the exception of those containing two 1,2,4-triazole groups, are superior in cytotoxic activity to the original phaeosphaeride and the positive control, etoposide.
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