Chromenopyrrole derivatives with multiple stereocenters and variable ring fusion pattern are found in many natural products and biologically appealing molecules. By employing a build/couple/pair strategy, we have recently reported on the discovery of a serendipitous cascade to access a diverse collection of chromenopyrroles. This protocol features a one-pot cascade that includes the generation of azomethine ylide and intramolecular [3 + 2]-cycloaddition. Phenotypic screening of the developed pilot library enabled the identification of chemical probes that efficiently suppress mitochondrial membrane potential, elevate reactive oxygen species content, and deplete ATP content in a hepatoma cell line (Hepa1-6), without affecting the proliferation of T- or B-cells. This selective targeting represents a new approach for the treatment of cancer.

在许多天然产物和具有生物吸引力的分子中发现具有多个立体中心和可变环稠合模式的铬吡咯衍生物。通过采用构建/配对/配对策略，我们最近报告了偶然级联的发现，以访问各种各样的苯并吡咯。该协议具有一锅级联的功能，其中包括产生甲亚胺叶立德和分子内[3 + 2]-环加成反应。通过对已开发的试验库进行表型筛选，可以鉴定能够有效抑制肝癌细胞系（Hepa1-6）中线粒体膜电位，提高活性氧含量和耗尽ATP含量的化学探针，而不会影响T-或B的增殖-细胞。这种选择性靶向代表了一种新的癌症治疗方法。