Enhancing the Structural Diversity and Bioactivity of Natural Products by Combinatorial Modification Exemplified by Total Tanshinones

To enhance the structural diversity of tanshinones and provide more derivatives for the biological studies, a one-pot combinatorial modification strategy was performed on total tanshinones. Six new quinoxlinetanshinones 1 – 6 were subsequently isolated from the combinatorial modified semi-synthetic mixture. The structures were elucidated by spectroscopic analysis in combination with single-crystal X-ray diffraction. These quinoxlinetanshinones demonstrated strong DNA binding properties. Rapid synthesis of new quinoxlinetanshinones with significant biological activity highlights the great potential of one-pot combinatorial modification for the diversification of natural products.