Potent but ill researched. Despite promising antiproliferative data of substituted xanthones, their structure-activity relationship remains largely unknown. We systematically synthesized previously inaccessible phenyl- and chloro-bearing xanthones through a modular chlorination followed by a concise and optimized sequence of polar condensation, cyclization and Suzuki coupling. Despite their simplicity several of these xanthones exhibited antiproliferative activities comparable to anticancer drug doxorubicin.

中文翻译：

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新型氧杂蒽酮的多样性导向合成揭示了有效的阿霉素类似物

有效但研究不足。尽管取代氧杂蒽酮的抗增殖数据有希望，但它们的结构-活性关系仍然很大程度上未知。我们通过模块化氯化，然后是简洁且优化的极性缩合、环化和铃木偶联序列，系统地合成了以前无法获得的含苯基和含氯的呫吨酮。尽管这些氧杂蒽酮很简单，但其中几种表现出与抗癌药物阿霉素相当的抗增殖活性。