| 摘要 |
A process for the total synthesis of thiocoraline and BE-22179 establishes the relative and absolute stereochemistry of these compounds and enables the construction and characterization of a series of related analogues (see Figure 4). The mechanism for the bioactivity of thiocoraline, BE-22179 and their related analogues is charaterized. Thiocoraline, BE-22179, and their related analogues are disclosed to bind to DNA by high-affinity bisintercalation and are disclosed to exhibit exceptional cytotoxic activity.
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