A new class of light‐harvesting dendrimers based on metal–organic hybrids (see picture) is described, including the synthesis and photophysical characterization. The inorganic core displays sensitized emission with decay times on the microsecond timescale, which is beneficial for fluorescence lifetime‐based technologies.
Pyruvate dehydrogenase kinase 1 (PDK1) is overexpressed in ovarian cancer and thus is a promising anticancer therapeutic target. Our previous work suggests that coumarin compounds are potential inhibitors of PDKs. In this study, we used the ovarian cancer cell line SKOV3 as the model system and examined whether dicumarol (DIC), a coumarin compound, could inhibit ovarian cancer through targeting PDK1. We showed that DIC potently inhibited the kinase activity of PDK1, shifted the glucose metabolism from aerobic glycolysis to oxidative phosphorylation, generated a higher level of reactive oxygen species (ROS), attenuated the mitochondrial membrane potential (MMP), induced apoptosis, and reduced cell viability in vitro. The same phenotypes induced by DIC also were translated in vivo, leading to significant suppression of xenograft growth. This study not only identifies a novel inhibitor for PDK1, but it also reveals novel anticancer mechanisms of DIC and provides a promising anticancer therapy that targets the Warburg effect.
Dearomatization reactions provide the most efficient method for the synthesis of spiro- or fused-ring systems from readily available compounds. This review summarizes the recent developments in dearomatization reactions of indoles, pyridines, quinolines, isoquinolines, and some other heteroaromatic compounds. The applications of these methods in total synthesis of natural products are also briefly introduced.
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