A three-step synthesis from rebeccamycin of an efficient checkpoint kinase 1 inhibitor

Rebeccamycin derivative 1 bearing a sugar moiety linked to both indole nitrogens and an amino substituent on the carbohydrate unit was synthesized in three steps from the bacterial metabolite. This compound was found to be a highly potent checkpoint kinase 1 inhibitor with an IC50 value of 2.8 nM.

Figure optionsDownload as PowerPoint slide