Aporphinoid alkaloids, which encompass a large number of complicated structures, are an important group of
natural products. The anticancer activity of aporphinoid alkaloids has become a hot pharmaceutical research area in recent
years. Recent studies on the anticancer activity of these compounds are reviewed. The structure activity relationships
(SARs) and anticancer mechanisms of aporphinoid alkaloids, as well as simple aporphine, oxoaporphine, dehydroaporphine
and dimeric aporphine, have been summarized. The presence of a 1,2-methylenedioxy group and methylation of nitrogen
are key features to the cytotoxicity of aporphinoid alkaloids. Oxidation and dehydrogenation of C7 could improve
the anticancer activity. The contributions of chirality of hydrogen at C6a and the substitution pattern of other positions
about aporphinoid alkaloids for anticancer activity remain unknown. Induced cancer cells apoptosis, prevention of cell
proliferation, DNA topoisomerase inhibition, reducing the drug-resistant cellular side population (SP) or cancer stem cells
(CSCs) and inhibition of epidermal growth factor receptor (EGFR) tyrosine kinase seem to play important roles in the molecular
mechanisms of anticancer activity about aporphinoid alkaloids.
Keywords: Natural product, Aporphinoid alkaloids, Chemical structure, Anticancer activity, Apoptosis, SARs.
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